Home Protein Tyrosine Kinase PDGFR inhibitor - c-Kit inhibitor - VEGFR inhibitor - IRE1 inhibitor - Autophagy activator - Apoptosis related activator Sunitinib For research use only.

Sunitinib

Synonyms: SU11248

Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.

Sunitinib Chemical Structure

Sunitinib Chemical Structure

CAS No. 557795-19-4

Purity & Quality Control

Sunitinib Related Products

Signaling Pathway

PDGFR Signaling Pathways

PDGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cell Function assay 24 h Inhibition of VEGF-A induced HUVEC cell sprouting after 24 hrs by angiogenesis assay, IC50=0.12 μM 21741249
HEK293 Function assay Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd = 0.00047 μM. 19754199
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM. 27077705
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.002 μM. 27077705
MV4-11 Cytotoxicity assay 72 hrs Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay, IC50 = 0.003 μM. 22452518
MV411 Antiproliferative assay 48 hrs Antiproliferative activity against human MV411 cells after 48 hrs by MTT assay, IC50 = 0.003 μM. 24904961
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.004 μM. 30204441
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay, IC50 = 0.0043 μM. 19754199
MV4-11 Cytotoxicity assay 72 hrs Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay, IC50 = 0.0043 μM. 19654408
Sf21 Function assay 60 mins Inhibition of recombinant human N-terminal His6-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells after 60 mins by ELISA, IC50 = 0.0047 μM. 30241010
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.005 μM. 30204441
MOLM14 Antiproliferative assay 72 hrs Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.005 μM. 27077705
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.006 μM. 30204441
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.006 μM. 27077705
MDA-MB-468 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.0061 μM. 24890652
3T3 Function assay Inhibition of PDGF-induced BrdU incorporation in 3T3 cells without bovine serum albumin, IC50 = 0.007 μM. 12646019
3T3 Function assay Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin, IC50 = 0.007 μM. 12646019
3T3 Function assay Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.5% bovine serum albumin, IC50 = 0.007 μM. 12646019
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM. 30204441
3T3 Function assay Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 1% bovine serum albumin, IC50 = 0.008 μM. 12646019
3T3 Function assay Inhibition of PDGF-induced BrdU incorporation in 3T3 cells, IC50 = 0.008 μM. 12646019
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay, IC50 = 0.009 μM. 20570526
MV4-11 Cytotoxicity assay Cytotoxicity against human MV4-11 cells by MTT assay, IC50 = 0.009 μM. 20833039
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.009 μM. 27077705
endothelial precursor cells Function assay Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay, IC50 = 0.0096 μM. 22409666
MDA-MB-435 Cytotoxicity assay Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.0097 μM. 24890652
RS4-11 Function assay 2 hrs Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay, IC50 = 0.0099 μM. 19654408
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50 = 0.01 μM. 29935772
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.012 μM. 30204441
Kasumi-1 Antiproliferative assay 72 hrs Antiproliferative activity against human Kasumi-1 cells after 72 hrs by MTT assay, IC50 = 0.016 μM. 20570526
RS4-11 Function assay Inhibition of FLT3 autophosphorylation in human RS4-11 cells by Western blot analysis, IC50 = 0.016 μM. 20833039
4T1 Cytotoxicity assay Cytotoxicity against mouse triple negative 4T1 cells, IC50 = 0.016 μM. 24890652
MOLM13 Cytotoxicity assay 48 hrs Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0177 μM. 25089810
NIH3T3 Function assay 1 hr Inhibitory concentration against human KDR kinase expressed in NIH3T3 cells with 4 uM Biotin-Ahx-AEEEYFFLFA-amide at ambient temperature for 1 hr, IC50 = 0.018 μM. 16162008
U251 Function assay Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50 = 0.0189 μM. 24900865
U251 Function assay Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay, IC50 = 0.0189 μM. 24890652
U251 Function assay 60 mins Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA, IC50 = 0.0189 μM. 30098869
U251 Function assay 60 mins Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method, IC50 = 0.0189 μM. 27894589
U251 Function assay 60 min Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0189 μM. 25882519
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.02 μM. 27077705
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.0223 μM. 24890652
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.023 μM. 27077705
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.024 μM. 30204441
MV4-11 Cytotoxicity assay 48 hrs Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0243 μM. 25089810
BA/F3 Function assay 72 hrs Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.027 μM. 30204441
MCF7 Cytotoxicity assay Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0271 μM. 24890652
MCF7 Cytotoxicity assay Cytotoxicity against human taxoid-resistant MCF7 cells, IC50 = 0.0293 μM. 24890652
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM. 22221201
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM. 22221201
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.03 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM. 30204441
RS4-11 Function assay 2 hrs Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay, IC50 = 0.034 μM. 19654408
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0368 μM. 25089810
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay, IC50 = 0.0385 μM. 28038328
TT Antiproliferative assay 72 hrs Antiproliferative activity against human TT cells pretreated for 72 hrs followed by compound-washout measured after 72 hrs by MTT assay, IC50 = 0.04 μM. 24904961
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.04 μM. 28991465
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.041 μM. 27077705
THP1 Cytotoxicity assay 48 hrs Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0457 μM. 25089810
3T3 Function assay Inhibition of Vascular endothelial growth factor receptor in 3T3 cells, IC50 = 0.05 μM. 12646019
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.053 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.078 μM. 27077705
3T3 Function assay Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 5% bovine serum albumin, IC50 = 0.083 μM. 12646019
SH-SY5Y Function assay Inhibition of PDGFRbeta in human SH-SY5Y cells by phosphotyrosine ELISA assay, IC50 = 0.0831 μM. 24890652
SH-SY5Y Function assay 60 mins Inhibition of PDGF-BB-induced PDGFRbeta activation in human SH-SY5Y cells pretreated for 60 mins followed by PDGF-BB addition and measured after 10 mins by ELISA, IC50 = 0.0831 μM. 30098869
SF539 Function assay 60 mins Inhibition of PDGFR-beta in human SF539 cells assessed as reduction in PDGF-BB induced phosphorylation preincubated for 60 mins followed by PDGF-BB addition measured after 10 mins by ELISA method, IC50 = 0.0831 μM. 27894589
U251 Function assay 60 min Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0831 μM. 25882519
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.09 μM. 28991465
GIST430 Cytotoxicity assay 72 hrs Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.098 μM. 28991465
HAEC Antiproliferative assay 72 hrs Antiproliferative activity against human HAEC cells expressing VEGFR after 72 hrs by MTT assay, IC50 = 0.1 μM. 22444679
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.11 μM. 27077705
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM. 30204441
FDC-P1 Function assay 48 hrs Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50 = 0.155 μM. 20156689
A431 Function assay Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA assay, IC50 = 0.1721 μM. 24890652
A431 Function assay 60 mins Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA, IC50 = 0.1721 μM. 30098869
A431 Function assay 60 mins Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.1721 μM. 25882519
Sf9 Function assay Inhibition of GST-tagged VEGFR expressed in Sf9 cells, IC50 = 0.185 μM. 19854051
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.214 μM. 30204441
BaPTC2 Growth inhibition assay 72 hrs Growth inhibition of mouse BaPTC2 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting, IC50 = 0.22 μM. 20117004
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.271 μM. 30204441
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against VEGFR expressing human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.33 μM. 23131541
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells expressing VEGFR after 72 hrs by MTT assay, IC50 = 0.33 μM. 22444679
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.398 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.43 μM. 30204441
THP1 Antiproliferative assay 72 hrs Antiproliferative activity against human THP1 cells after 72 hrs by MTT assay, IC50 = 0.5 μM. 20570526
CHO Function assay Inhibition of human ERG expressed in CHO cells by Qpatch assay, IC50 = 0.5 μM. 28038328
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.51 μM. 27077705
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.584 μM. 30204441
CAKI-1 Antiproliferative assay 48 hrs Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay, GI50 = 0.63 μM. 22560627
BA/F3 Function assay 72 hrs Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.631 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.638 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.696 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.782 μM. 30204441
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by MTT assay, IC50 = 0.83 μM. 24904961
Rec1 Antiproliferative assay 72 hrs Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.87 μM. 27077705
RS4:11 Antiproliferative assay 72 hrs Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay, IC50 = 1 μM. 20570526
K562 Antiproliferative assay 72 hrs Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1 μM. 27077705
NCI-H526 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H526 cells after 72 hrs by MTT assay, IC50 = 1.01 μM. 24904961
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 1.1 μM. 22221201
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.1 μM. 27077705
BA/F3 Growth inhibition assay 72 hrs Growth inhibition of mouse BA/F3 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting, IC50 = 1.2 μM. 20117004
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.2 μM. 27077705
Sf9 Function assay Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells, IC50 = 1.3 μM. 20117004
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 1.3 μM. 21621880
SW620 Antiproliferative assay 48 hrs Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay, GI50 = 1.3 μM. 22560627
IM9 Antitumor assay Antitumor activity against human IM9 cells, IC50 = 1.35 μM. 21450463
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.38 μM. 27077705
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 1.47 μM. 23999040
HT-29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay, GI50 = 1.6 μM. 22560627
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 1.7 μM. 26920800
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.7 μM. 27077705
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 2 μM. 22560627
MDA-MB-435 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay, GI50 = 2 μM. 22560627
GIST48B Antiproliferative assay 72 hrs Antiproliferative activity against human GIST48B cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.01 μM. 27077705
CHO Antiproliferative assay 72 hrs Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.03 μM. 27077705
KB-3-1 Cytotoxicity assay 72 hrs Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay, IC50 = 2.3 μM. 19397322
K562 Antitumor assay Antitumor activity against human K562 cells, IC50 = 2.41 μM. 21450463
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 2.44 μM. 23602441
T24 Antiproliferative assay 72 hrs Antiproliferative activity against human T24 cells after 72 hrs by MTT assay, IC50 = 2.44 μM. 23999040
CHL Antiproliferative assay 72 hrs Antiproliferative activity against CHL cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.48 μM. 27077705
ACHN Cytotoxicity assay 6 days Cytotoxicity against human ACHN cells assessed as inhibition of cell viability after 6 days by MTT assay, IC50 = 2.5 μM. 23360104
Bel7402 Antiproliferative assay 72 hrs Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50 = 2.67 μM. 24904961
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 2.7 μM. 21621880
BAF3 Antiproliferative assay Antiproliferative activity against mouse BAF3 cells, GI50 = 2.78 μM. 27077705
HuH7 Antiproliferative assay Antiproliferative activity against human HuH7 cells by MTT assay, IC50 = 3.03 μM. 30059803
HuH7 Growth inhibition assay 48 hrs Growth inhibition of human HuH7 cells after 48 hrs by MTT assay, IC50 = 3.03 μM. 27956344
OVCAR3 Antiproliferative assay 48 hrs Antiproliferative activity against human OVCAR3 cells after 48 hrs by SRB assay, GI50 = 3.2 μM. 22560627
HL60 Antitumor assay Antitumor activity against human HL60 cells, IC50 = 3.53 μM. 21450463
BxPC3 Antiproliferative assay 72 hrs Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay, IC50 = 3.63 μM. 23999040
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 3.7 μM. 21621880
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 3.81 μM. 20570526
UACC257 Antiproliferative assay 48 hrs Antiproliferative activity against human UACC257 cells after 48 hrs by SRB assay, GI50 = 4 μM. 22560627
RCC4 Anticancer assay 48 hrs Anticancer activity against human RCC4 cells after 48 hrs by XTT assay, IC50 = 4 μM. 28325600
KBV1 Cytotoxicity assay 72 hrs Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay, IC50 = 4.1 μM. 19397322
A498 Cytotoxicity assay 72 hrs Cytotoxicity against human A498 cells after 72 hrs by MTT assay, IC50 = 4.3 μM. 23489626
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 4.31 μM. 24904961
MDA-MB-231 Antitumor assay Antitumor activity against human MDA-MB-231 cells, IC50 = 4.51 μM. 21450463
L02 Cytotoxicity assay 72 hrs Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay, IC50 = 4.62 μM. 27643639
HT-29 Cytotoxicity assay 48 hrs Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 4.7 μM. 26009164
HuH7 Antiproliferative assay 48 hrs Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.707 μM. 29057042
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 4.71 μM. 23602441
BGC Antiproliferative assay 72 hrs Antiproliferative activity against human BGC cells after 72 hrs by MTT assay, IC50 = 4.78 μM. 23999040
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 4.789 μM. 30204441
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay, IC50 = 4.95 μM. 27643639
A375 Toxicity against 72 hrs Toxicity against human A375 cells after 72 hrs by cell titer-blue assay, IC50 = 5.4 μM. 19654408
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 5.61 μM. 23999040
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 5.62 μM. 30059803
HCT116 Growth inhibition assay 48 hrs Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50 = 5.62 μM. 27956344
ACHN Cytotoxicity assay 72 hrs Cytotoxicity against human ACHN cells after 72 hrs by MTT assay, IC50 = 5.7 μM. 23489626
HK2 Antiproliferative assay 72 hrs Antiproliferative activity against human HK2 cells after 72 hrs by MTT assay, IC50 = 5.85 μM. 24904961
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 5.88 μM. 28991465
MDA-MB-231 Anticancer assay 48 hrs Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay, IC50 = 6 μM. 28325600
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 6.1 μM. 22019188
HEK293 Function assay 2 mins Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay, IC50 = 6.1 μM. 28230985
SW620 Antiproliferative assay Antiproliferative activity against human SW620 cells by MTT assay, IC50 = 6.25 μM. 30059803
SW620 Growth inhibition assay 48 hrs Growth inhibition of human SW620 cells after 48 hrs by MTT assay, IC50 = 6.25 μM. 27956344
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 6.29 μM. 23602441
TK10 Antiproliferative assay 48 hrs Antiproliferative activity against human TK10 cells after 48 hrs by SRB assay, GI50 = 6.3 μM. 22560627
SMMC7721 Cytotoxicity assay 72 hrs Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 6.47 μM. 21621880
A549 Antitumor assay Antitumor activity against human A549 cells, IC50 = 6.61 μM. 21450463
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 6.98 μM. 28760313
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 7.4 μM. 27128173
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 7.4 μM. 27639369
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 7.44 μM. 27448916
HepG2 Antiproliferative assay Antiproliferative activity against human HepG2 cells by MTT assay, IC50 = 7.78 μM. 30059803
EKVX Antiproliferative assay 48 hrs Antiproliferative activity against human EKVX cells after 48 hrs by SRB assay, GI50 = 7.9 μM. 22560627
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 7.93 μM. 26009164
CHO Function assay Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform, IC50 = 7.94328 μM. 25087753
PA1 Cytotoxicity assay 48 hrs Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 7.97 μM. 27210438
A498 Antiproliferative assay 48 hrs Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 7.981 μM. 29057042
COLO205 Cytotoxicity assay 24 hrs Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay, IC50 = 8 μM. 28756024
SVEC4-10 Cytotoxicity assay 24 hrs Cytotoxicity against mouse SVEC4-10 cells assessed as cell viability after 24 hrs by MTS assay, IC50 = 8 μM. 26912111
WI38 Cytotoxicity assay 72 hrs Cytotoxicity against human WI38 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 8.56 μM. 21621880
A549 Cytotoxicity assay Cytotoxicity against human A549 cells by MTT assay, IC50 = 9.1 μM. 26920800
SKOV3 Cytotoxicity assay 48 hrs Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 9.21 μM. 26009164
MDA-MB-435 Cytotoxicity assay Cytotoxicity against human MDA-MB-435 cells by MTT assay, IC50 = 9.3 μM. 26920800
SNB19 Antiproliferative assay 48 hrs Antiproliferative activity against human SNB19 cells after 48 hrs by SRB assay, GI50 = 10 μM. 22560627
CHO K1 Function assay Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform, IC50 = 10 μM. 25087753
NCI-H727 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 10.12 μM. 29057042
HeLa Cytotoxicity assay 48 hrs Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 10.4 μM. 27639369
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 10.5 μM. 25064347
PC9 Cytotoxicity assay 48 hrs Cytotoxicity against human PC9 cells after 48 hrs by MTT assay, IC50 = 10.97 μM. 22483608
Bel7402 Photocytotoxicity assay 5 hrs Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 11 μM. 26584085
A375 Cytotoxicity assay 48 hrs Cytotoxicity against human A375 cells after 48 hrs by MTT assay, IC50 = 11.58 μM. 22483608
SF539 Function assay 10 mins Inhibition of PDGFRbeta phosphorylation in human SF539 cells after 10 mins by FLISA, IC50 = 12.2 μM. 20403700
A431 Function assay Inhibition of PDGFRbeta expressed in human A431 cells, IC50 = 12.2 μM. 20558072
SF-539 Function assay 60 mins Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells after 60 mins by ELISA, IC50 = 12.2 μM. 22204741
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 12.35 μM. 22483608
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 12.6 μM. 27639369
LNCAP Cytotoxicity assay 48 hrs Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 12.61 μM. 27210438
PANC1 Photocytotoxicity assay 5 hrs Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 13 μM. 26584085
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 13.24 μM. 22483608
endothelial precursor cells Function assay Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay, IC50 = 13.6 μM. 22409666
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 13.6 μM. 25064347
K562 Cytotoxicity assay 24 hrs Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50 = 14 μM. 28756024
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 14.4 μM. 27448916
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 14.4 μM. 27639369
PANC1 Cytotoxicity assay 48 hrs Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 14.94 μM. 26009164
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 15.4 μM. 22019188
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 15.5 μM. 22019188
BT549 Cytotoxicity assay 48 hrs Cytotoxicity against human BT549 cells after 48 hrs by MTT assay, IC50 = 15.5 μM. 27128173
BT549 Cytotoxicity assay 48 hrs Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 15.5 μM. 27639369
BT549 Cytotoxicity assay 48 hrs Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 15.54 μM. 27448916
CHO K1 Function assay Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 15.8489 μM. 25087753
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 16.06 μM. 28057423
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 16.06 μM. 26009164
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 16.3 μM. 27639369
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 16.38 μM. 27448916
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells after 48 hrs by MTT assay, IC50 = 16.4 μM. 27128173
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 18.35 μM. 22483608
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 18.5 μM. 22019188
U251 Function assay 10 mins Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA, IC50 = 18.9 μM. 20403700
A431 Function assay Inhibition of VEGFR2 expressed in human A431 cells, IC50 = 18.9 μM. 20558072
U251 Function assay 60 mins Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA, IC50 = 18.9 μM. 22204741
U251 Function assay 60 mins Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 18.9 μM. 23375090
U251 Function assay 60 mins Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA, IC50 = 18.9 μM. 23434139
U251 Function assay 60 mins Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 18.9 μM. 22739090
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 19.6 μM. 27128173
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 19.6 μM. 27448916
LO2 Antiproliferative assay 72 hrs Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay, IC50 = 19.93 μM. 24904961
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50 = 21.9 μM. 22019188
RWPE1 Cytotoxicity assay 48 hrs Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23 μM. 27210438
RWPE1 Cytotoxicity assay 48 hrs Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay, IC50 = 23 μM. 27128173
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23.76 μM. 27210438
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 23.8 μM. 27448916
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 25.1 μM. 22019188
RWPE1 Cytotoxicity assay 48 hrs Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 25.2 μM. 27639369
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 25.41 μM. 28057423
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 25.41 μM. 26009164
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 32 μM. 28756024
CHO Function assay Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 33.4 μM. 23812503
HEK293 Function assay Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 39.8107 μM. 25087753
H4 Toxicity assay 10 uM Toxicity in human H4 cells at 10 uM, Activity = 40 μM. 20350806
MV4-11 Antitumor assay 30 mg/kg 28 days Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as suppression of tumor volume at 30 mg/kg, po QD for 28 days measured after dosing period 19754199
MV4-11 Antitumor assay 30 mg/kg 28 days Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as tumor growth regression at 30 mg/kg, po QD for 28 days measured after dosing period 19754199
MV4-11 Antitumor assay 30 mg/kg 28 days Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 30 mg/kg, po QD for 28 days measured during first 14 days of dosing 19754199
SK-RC-52 Antitumor assay 20 mg/kg Antitumor activity against human SK-RC-52 cells xenografted BALB/c nu/nu mouse assessed as inhibition of tumor growth at 20 mg/kg, ip 19615903
MV411 Antitumor assay 10 mg/kg 28 days Antitumor activity against human MV411 cells in xenografted athymic nude mouse model assessed as decrease in tumor size at 10 mg/kg, po qd for 28 days measured after 29 to 36 days 19646870
MV411 Antitumor assay 30 mg/kg 28 days Antitumor activity against human MV411 cells in xenografted athymic nude mouse model assessed as decrease in tumor size at 30 mg/kg, po qd for 28 days 19646870
MV4-11 Antitumor assay 10 mg/kg Antitumor activity against human MV4-11 cells xenografted mouse model assessed as inhibition of tumor growth at at 10 mg/kg, po 19654408
HEK293 Function assay 100 nM 1 hr Inhibition of VEGF-induced autophosphorylation of tyrosine 1175 residue on VEGFR2 expressed in HEK293 cells at 100 nM after 1 hr by ELISA 21885287
Calu6 Antitumor assay 80 mg/kg 11 days Antitumor activity against human Calu6 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 80 mg/kg, po qd for 11 days 22269278
BA/F3 Antitumor assay 0.05 to 5 mg/kg 100 days Antitumor activity against mouse BA/F3 cells expressing FLT3-ITD mutant xenografted in BALB/c mouse myeloproliferative model assessed as disease related death at 0.05 to 5 mg/kg, po measured after 100 days 22221201
MDA-MB-435 Antiangiogenic assay 20 mg/kg 2 days Antiangiogenic activity in human MDA-MB-435 cells xenografted in chicken embryo chorioallantoic membrane assessed as inhibition of blood vessel formation at 20 mg/kg measured after 2 days 23664876
MDA-MB-435 Antitumor assay 20 mg/kg 2 days Antitumor activity against human MDA-MB-435 cells xenografted in chicken embryo chorioallantoic membrane assessed as inhibition of tumor volume at 20 mg/kg measured after 2 days 23664876
U251 Antitumor assay 30 mg/kg up to 34 days Antitumor activity against human U251 cells xenografted into athymic NCr mouse assessed as decrease in tumor growth at 30 mg/kg twice weekly measured up to 34 days 24900865
MDA-MB-435 Antitumor assay 30 mg/kg up to 34 days Antitumor activity against human MDA-MB-435 cells xenografted into flank of athymic BALBc/J mouse assessed as decrease in tumor growth at 30 mg/kg twice weekly measured up to 34 days 24900865
MDA-MB-435 Antitumor assay 30 mg/kg Antitumor activity against human MDA-MB-435 cells xenografted into flank of athymic BALBc/J mouse assessed as decrease in tumor vascular density at 30 mg/kg twice weekly by CD31/PECAM-1 immunohistochemical staining 24900865
NCI-H460 Antitumor assay 40 mg/kg up to 21 days Antitumor activity against human NCI-H460 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 40 mg/kg/day administered qd measured up to day 21 relative to control 24904961
HT-29 Antitumor assay 40 mg/kg up to 21 days Antitumor activity against human HT-29 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 80 mg/kg/day administered qd measured up to day 21 relative to control 24904961
MCF7 Function assay 4 uM 24 hrs Inhibition of VEGFR2 phosphorylation in human MCF7 cells at 4 uM incubated for 24 hrs by Western blot method 28942113
HUVEC Antiangiogenic assay 10 uM 5 hrs Antiangiogenic activity in human HUVEC cells assessed as angiogenesis rate at 10 uM after 5 hrs by endothelial tube formation assay relative to control 26912111
MCF7 Function assay 1 uM 24 hrs Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated ERK1/2 at 1 uM incubated for 24 hrs by Western blot analysis 27176944
MCF7 Function assay 1 uM 24 hrs Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated Raf1 at 1 uM incubated for 24 hrs by Western blot analysis 27176944
HCT116 Antimigratory assay 24 hrs Antimigratory activity against human HCT116 cells assessed as inhibition of cell migration after 24 hrs by wound healing assay 23153200
U87MG Function assay 10 mg/kg 3 days In-vivo inhibition of angiogenesis in human U87MG cells xenografted in athymic nude Harlan mouse at 10 mg/kg oral gavage dosed twice daily for 3 days measured 3 days post dose by fluorescence microscopy 22409666
EoL-1-cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50 = 0.0000016 μM. SANGER
MV-4-11 Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50 = 0.0002722 μM. SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50 = 0.0153 μM. SANGER
CGTH-W-1 Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 0.03094 μM. SANGER
MONO-MAC-6 Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50 = 0.0338 μM. SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 0.07989 μM. SANGER
NKM-1 Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50 = 0.09852 μM. SANGER
KM12 Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50 = 0.35014 μM. SANGER
TE-15 Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50 = 0.50761 μM. SANGER
697 Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50 = 0.61425 μM. SANGER
MOLT-16 Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 0.63132 μM. SANGER
GB-1 Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay, IC50 = 0.71023 μM. SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 0.80455 μM. SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 0.98106 μM. SANGER
LC-2-ad Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50 = 1.11407 μM. SANGER
BL-70 Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50 = 1.11846 μM. SANGER
ETK-1 Growth inhibition assay Inhibition of human ETK-1 cell growth in a cell viability assay, IC50 = 1.2858 μM. SANGER
A4-Fuk Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 1.34141 μM. SANGER
OCI-AML2 Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50 = 1.36851 μM. SANGER
SIG-M5 Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50 = 1.37009 μM. SANGER
NCI-SNU-16 Growth inhibition assay Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50 = 1.46486 μM. SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 1.50676 μM. SANGER
SR Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50 = 1.54572 μM. SANGER
A3-KAW Growth inhibition assay Inhibition of human A3-KAW cell growth in a cell viability assay, IC50 = 1.62546 μM. SANGER
KS-1 Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50 = 1.69247 μM. SANGER
CTV-1 Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50 = 1.72751 μM. SANGER
LB1047-RCC Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 1.81624 μM. SANGER
MEG-01 Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 1.83563 μM. SANGER
TE-11 Growth inhibition assay Inhibition of human TE-11 cell growth in a cell viability assay, IC50 = 1.83985 μM. SANGER
CMK Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50 = 1.95517 μM. SANGER
NB1 Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50 = 1.96117 μM. SANGER
HAL-01 Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 2.05946 μM. SANGER
DEL Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50 = 2.08482 μM. SANGER
RL95-2 Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50 = 2.11137 μM. SANGER
KARPAS-299 Growth inhibition assay Inhibition of human KARPAS-299 cell growth in a cell viability assay, IC50 = 2.11313 μM. SANGER
EW-16 Growth inhibition assay Inhibition of human EW-16 cell growth in a cell viability assay, IC50 = 2.13508 μM. SANGER
RS4-11 Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 2.17924 μM. SANGER
BB30-HNC Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50 = 2.22375 μM. SANGER
DOHH-2 Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50 = 2.33431 μM. SANGER
RPMI-8402 Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50 = 2.33618 μM. SANGER
BV-173 Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 2.3366 μM. SANGER
TE-10 Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50 = 2.34384 μM. SANGER
TE-8 Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50 = 2.37038 μM. SANGER
K052 Growth inhibition assay Inhibition of human K052 cell growth in a cell viability assay, IC50 = 2.40202 μM. SANGER
KARPAS-45 Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50 = 2.49446 μM. SANGER
SK-NEP-1 Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 2.60237 μM. SANGER
KGN Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50 = 2.60339 μM. SANGER
ML-2 Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50 = 2.63512 μM. SANGER
LAMA-84 Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 2.69545 μM. SANGER
LXF-289 Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50 = 2.72989 μM. SANGER
A101D Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50 = 2.78304 μM. SANGER
KY821 Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50 = 2.79758 μM. SANGER
ES4 Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay, IC50 = 2.80628 μM. SANGER
SCC-3 Growth inhibition assay Inhibition of human SCC-3 cell growth in a cell viability assay, IC50 = 2.82891 μM. SANGER
NALM-6 Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50 = 2.90473 μM. SANGER
BL-41 Growth inhibition assay Inhibition of human BL-41 cell growth in a cell viability assay, IC50 = 2.91222 μM. SANGER
OPM-2 Growth inhibition assay Inhibition of human OPM-2 cell growth in a cell viability assay, IC50 = 3.05954 μM. SANGER
SF126 Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50 = 3.06198 μM. SANGER
BE-13 Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 3.23111 μM. SANGER
SF268 Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50 = 3.32869 μM. SANGER
MOLT-4 Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 3.39838 μM. SANGER
PF-382 Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50 = 3.4457 μM. SANGER
HEL Growth inhibition assay Inhibition of human HEL cell growth in a cell viability assay, IC50 = 3.48005 μM. SANGER
RPMI-6666 Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50 = 3.54171 μM. SANGER
QIMR-WIL Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 3.63391 μM. SANGER
ATN-1 Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50 = 3.67114 μM. SANGER
BB49-HNC Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50 = 3.70508 μM. SANGER
HCE-4 Growth inhibition assay Inhibition of human HCE-4 cell growth in a cell viability assay, IC50 = 3.78642 μM. SANGER
SK-LMS-1 Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50 = 3.83338 μM. SANGER
MS-1 Growth inhibition assay Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 3.83778 μM. SANGER
JAR Growth inhibition assay Inhibition of human JAR cell growth in a cell viability assay, IC50 = 3.98832 μM. SANGER
KE-37 Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50 = 4.06158 μM. SANGER
LB996-RCC Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50 = 4.12168 μM. SANGER
HH Growth inhibition assay Inhibition of human HH cell growth in a cell viability assay, IC50 = 4.20914 μM. SANGER
HL-60 Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50 = 4.21065 μM. SANGER
HOP-62 Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50 = 4.3352 μM. SANGER
NOMO-1 Growth inhibition assay Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50 = 4.33699 μM. SANGER
DU-4475 Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50 = 4.36729 μM. SANGER
LC4-1 Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50 = 4.3807 μM. SANGER
MC116 Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50 = 4.43081 μM. SANGER
SW982 Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay, IC50 = 4.55307 μM. SANGER
SK-N-DZ Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50 = 4.67099 μM. SANGER
EW-1 Growth inhibition assay Inhibition of human EW-1 cell growth in a cell viability assay, IC50 = 4.67911 μM. SANGER
SU-DHL-1 Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50 = 4.80174 μM. SANGER
L-363 Growth inhibition assay Inhibition of human L-363 cell growth in a cell viability assay, IC50 = 4.80621 μM. SANGER
OS-RC-2 Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50 = 4.8731 μM. SANGER
HD-MY-Z Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50 = 5.17301 μM. SANGER
MHH-PREB-1 Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50 = 5.32312 μM. SANGER
HC-1 Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay, IC50 = 5.43291 μM. SANGER
SK-MM-2 Growth inhibition assay Inhibition of human SK-MM-2 cell growth in a cell viability assay, IC50 = 5.4782 μM. SANGER
SH-4 Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50 = 5.4837 μM. SANGER
MHH-CALL-2 Growth inhibition assay Inhibition of human MHH-CALL-2 cell growth in a cell viability assay, IC50 = 5.76719 μM. SANGER
KG-1 Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50 = 6.02878 μM. SANGER
J-RT3-T3-5 Growth inhibition assay Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay, IC50 = 6.07909 μM. SANGER
MMAC-SF Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50 = 6.10949 μM. SANGER
IST-SL2 Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50 = 6.12519 μM. SANGER
SW954 Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 6.27517 μM. SANGER
HDLM-2 Growth inhibition assay Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50 = 6.32109 μM. SANGER
ST486 Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50 = 6.3471 μM. SANGER
DG-75 Growth inhibition assay Inhibition of human DG-75 cell growth in a cell viability assay, IC50 = 6.43069 μM. SANGER
EW-3 Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50 = 6.43207 μM. SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50 = 6.51507 μM. SANGER
GT3TKB Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 6.60763 μM. SANGER
KU812 Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50 = 6.6942 μM. SANGER
CESS Growth inhibition assay Inhibition of human CESS cell growth in a cell viability assay, IC50 = 7.10438 μM. SANGER
BC-1 Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50 = 7.24812 μM. SANGER
MZ1-PC Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50 = 7.30389 μM. SANGER
NCI-H82 Growth inhibition assay Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50 = 7.3785 μM. SANGER
NCI-H1355 Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50 = 7.45804 μM. SANGER
RPMI-8226 Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 7.50739 μM. SANGER
ARH-77 Growth inhibition assay Inhibition of human ARH-77 cell growth in a cell viability assay, IC50 = 7.53597 μM. SANGER
MN-60 Growth inhibition assay Inhibition of human MN-60 cell growth in a cell viability assay, IC50 = 7.54088 μM. SANGER
IMR-5 Growth inhibition assay Inhibition of human IMR-5 cell growth in a cell viability assay, IC50 = 7.54876 μM. SANGER
KARPAS-422 Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50 = 7.57206 μM. SANGER
CA46 Growth inhibition assay Inhibition of human CA46 cell growth in a cell viability assay, IC50 = 7.58012 μM. SANGER
SJSA-1 Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50 = 7.66061 μM. SANGER
no-11 Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50 = 7.77557 μM. SANGER
IST-SL1 Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50 = 8.02417 μM. SANGER
NCI-H209 Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50 = 8.11652 μM. SANGER
TALL-1 Growth inhibition assay Inhibition of human TALL-1 cell growth in a cell viability assay, IC50 = 8.18384 μM. SANGER
KMOE-2 Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50 = 8.1942 μM. SANGER
HCC1599 Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50 = 8.19987 μM. SANGER
GI-1 Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50 = 8.20411 μM. SANGER
NCI-H1304 Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay, IC50 = 8.20661 μM. SANGER
Daudi Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50 = 8.23546 μM. SANGER
CPC-N Growth inhibition assay Inhibition of human CPC-N cell growth in a cell viability assay, IC50 = 8.29199 μM. SANGER
MC-CAR Growth inhibition assay Inhibition of human MC-CAR cell growth in a cell viability assay, IC50 = 8.3358 μM. SANGER
SW872 Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50 = 8.34758 μM. SANGER
OVCAR-4 Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 8.50351 μM. SANGER
OCUB-M Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50 = 8.56508 μM. SANGER
SK-PN-DW Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50 = 8.60985 μM. SANGER
NCCIT Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50 = 8.71745 μM. SANGER
NCI-H1648 Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50 = 9.13834 μM. SANGER
COR-L279 Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50 = 9.3909 μM. SANGER
LS-123 Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50 = 9.68161 μM. SANGER
LP-1 Growth inhibition assay Inhibition of human LP-1 cell growth in a cell viability assay, IC50 = 9.78083 μM. SANGER
NB13 Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50 = 9.79994 μM. SANGER
ONS-76 Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50 = 9.81016 μM. SANGER
VA-ES-BJ Growth inhibition assay Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50 = 9.99933 μM. SANGER
GR-ST Growth inhibition assay Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 10.2207 μM. SANGER
ES1 Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 10.2984 μM. SANGER
NB14 Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50 = 10.9276 μM. SANGER
Ramos-2G6-4C10 Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 11.265 μM. SANGER
RXF393 Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50 = 11.4834 μM. SANGER
NCI-H2107 Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50 = 11.5984 μM. SANGER
K-562 Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay, IC50 = 11.8702 μM. SANGER
LOUCY Growth inhibition assay Inhibition of human LOUCY cell growth in a cell viability assay, IC50 = 11.9875 μM. SANGER
TGBC1TKB Growth inhibition assay Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50 = 12.002 μM. SANGER
COLO-320-HSR Growth inhibition assay Inhibition of human COLO-320-HSR cell growth in a cell viability assay, IC50 = 12.1565 μM. SANGER
K5 Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50 = 12.2985 μM. SANGER
BC-3 Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay, IC50 = 12.4651 μM. SANGER
REH Growth inhibition assay Inhibition of human REH cell growth in a cell viability assay, IC50 = 12.6498 μM. SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50 = 12.6887 μM. SANGER
IST-MEL1 Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50 = 12.8695 μM. SANGER
NCI-H128 Growth inhibition assay Inhibition of human NCI-H128 cell growth in a cell viability assay, IC50 = 13.0723 μM. SANGER
NCI-H1694 Growth inhibition assay Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50 = 13.1144 μM. SANGER
TGW Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50 = 13.3276 μM. SANGER
NCI-SNU-1 Growth inhibition assay Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50 = 13.345 μM. SANGER
IST-MES1 Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50 = 13.6729 μM. SANGER
CTB-1 Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50 = 13.7294 μM. SANGER
HUTU-80 Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50 = 13.7573 μM. SANGER
LAN-6 Growth inhibition assay Inhibition of human LAN-6 cell growth in a cell viability assay, IC50 = 14.2457 μM. SANGER
KP-N-YS Growth inhibition assay Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 14.2894 μM. SANGER
CCRF-CEM Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50 = 14.4169 μM. SANGER
NCI-H1770 Growth inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay, IC50 = 14.5369 μM. SANGER
MZ2-MEL Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50 = 15.2251 μM. SANGER
COR-L88 Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50 = 16.0012 μM. SANGER
LOXIMVI Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50 = 16.256 μM. SANGER
KALS-1 Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50 = 16.5931 μM. SANGER
D-283MED Growth inhibition assay Inhibition of human D-283MED cell growth in a cell viability assay, IC50 = 16.8489 μM. SANGER
NCI-H719 Growth inhibition assay Inhibition of human NCI-H719 cell growth in a cell viability assay, IC50 = 16.9161 μM. SANGER
MLMA Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50 = 16.9907 μM. SANGER
EVSA-T Growth inhibition assay Inhibition of human EVSA-T cell growth in a cell viability assay, IC50 = 17.0485 μM. SANGER
SK-N-FI Growth inhibition assay Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50 = 17.6913 μM. SANGER
NTERA-S-cl-D1 Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 17.8572 μM. SANGER
NCI-H1882 Growth inhibition assay Inhibition of human NCI-H1882 cell growth in a cell viability assay, IC50 = 17.9834 μM. SANGER
A704 Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50 = 17.9904 μM. SANGER
L-428 Growth inhibition assay Inhibition of human L-428 cell growth in a cell viability assay, IC50 = 18.0151 μM. SANGER
HCC1187 Growth inhibition assay Inhibition of human HCC1187 cell growth in a cell viability assay, IC50 = 18.0188 μM. SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 18.0866 μM. SANGER
BB65-RCC Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50 = 18.4162 μM. SANGER
EM-2 Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50 = 18.5672 μM. SANGER
Raji Growth inhibition assay Inhibition of human Raji cell growth in a cell viability assay, IC50 = 19.9565 μM. SANGER
TE-1 Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 20.4104 μM. SANGER
SW962 Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay, IC50 = 20.4293 μM. SANGER
MHH-NB-11 Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50 = 20.5521 μM. SANGER
no-10 Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50 = 21.0265 μM. SANGER
GDM-1 Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50 = 21.9414 μM. SANGER
KMS-12-PE Growth inhibition assay Inhibition of human KMS-12-PE cell growth in a cell viability assay, IC50 = 22.2739 μM. SANGER
NCI-H510A Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50 = 24.1278 μM. SANGER
ES5 Growth inhibition assay Inhibition of human ES5 cell growth in a cell viability assay, IC50 = 24.7349 μM. SANGER
JiyoyeP-2003 Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50 = 26.2742 μM. SANGER
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50 = 27.1822 μM. SANGER
NCI-H446 Growth inhibition assay Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50 = 27.4946 μM. SANGER
NB7 Growth inhibition assay Inhibition of human NB7 cell growth in a cell viability assay, IC50 = 27.9229 μM. SANGER
A388 Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50 = 28.0073 μM. SANGER
JVM-2 Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50 = 28.2898 μM. SANGER
HT-144 Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50 = 28.6899 μM. SANGER
NCI-H747 Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 28.9195 μM. SANGER
NCI-H1650 Growth inhibition assay Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50 = 29.0176 μM. SANGER
EB-3 Growth inhibition assay Inhibition of human EB-3 cell growth in a cell viability assay, IC50 = 29.5309 μM. SANGER
KLE Growth inhibition assay Inhibition of human KLE cell growth in a cell viability assay, IC50 = 29.619 μM. SANGER
TK10 Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay, IC50 = 30.126 μM. SANGER
COLO-668 Growth inhibition assay Inhibition of human COLO-668 cell growth in a cell viability assay, IC50 = 30.792 μM. SANGER
NCI-H23 Growth inhibition assay Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50 = 31.1063 μM. SANGER
GOTO Growth inhibition assay Inhibition of human GOTO cell growth in a cell viability assay, IC50 = 31.6085 μM. SANGER
MSTO-211H Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50 = 31.8678 μM. SANGER
LB831-BLC Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50 = 32.3843 μM. SANGER
SCH Growth inhibition assay Inhibition of human SCH cell growth in a cell viability assay, IC50 = 32.8485 μM. SANGER
EHEB Growth inhibition assay Inhibition of human EHEB cell growth in a cell viability assay, IC50 = 34.1193 μM. SANGER
U-266 Growth inhibition assay Inhibition of human U-266 cell growth in a cell viability assay, IC50 = 34.2782 μM. SANGER
EW-11 Growth inhibition assay Inhibition of human EW-11 cell growth in a cell viability assay, IC50 = 34.4725 μM. SANGER
TE-9 Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50 = 37.0401 μM. SANGER
ES3 Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50 = 37.5004 μM. SANGER
NCI-H2141 Growth inhibition assay Inhibition of human NCI-H2141 cell growth in a cell viability assay, IC50 = 38.0843 μM. SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 42.0586 μM. SANGER
SK-MEL-2 Growth inhibition assay Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50 = 42.6405 μM. SANGER
LC-1F Growth inhibition assay Inhibition of human LC-1F cell growth in a cell viability assay, IC50 = 43.3682 μM. SANGER
NH-12 Growth inhibition assay Inhibition of human NH-12 cell growth in a cell viability assay, IC50 = 43.9359 μM. SANGER
RKO Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50 = 44.1252 μM. SANGER
KM-H2 Growth inhibition assay Inhibition of human KM-H2 cell growth in a cell viability assay, IC50 = 44.9577 μM. SANGER
SK-UT-1 Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50 = 49.8825 μM. SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Targets
FLT3 [1]
(Cell-free assay)		 c-Kit [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro
In vitro Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]
Kinase Assay Biochemical Tyrosine Kinase Assays
IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research Cell lines RS4;11, MV4;11, and OC1-AML5
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation Time 24 and 48 hours
Method

Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-ERK / ERK p-GSK3β / GSK3β / MYCN p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK 24759734
Growth inhibition assay Cell viability 24369536
In Vivo
In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]
Animal Research Animal Models Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
Dosages ~80 mg/kg
Administration Orally once daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06222593 Not yet recruiting
Carcinoma Renal Cell
State University of New York at Buffalo
 June 1 2024 Phase 1|Phase 2
NCT06208748 Not yet recruiting
Gastrointestinal Stromal Tumors|GIST
Sarcoma Alliance for Research through Collaboration|Cogent Biosciences Inc.|Dana-Farber Cancer Institute|The Life Raft Group
 March 2024 Phase 2
NCT05745142 Completed
Carcinoma Renal Cell|Clear-cell Metastatic Renal Cell Carcinoma
Pfizer
 February 23 2023 --
NCT05043090 Recruiting
Papillary Renal Cell Carcinoma
AstraZeneca
 October 28 2021 Phase 3
NCT04669366 Completed
Kidney Neoplasms
Pfizer
 January 20 2021 --

Chemical Information & Solubility

Molecular Weight 398.47 Formula

C22H27FN4O2
CAS No. 557795-19-4 SDF Download Sunitinib SDF
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 25 mg/mL ( (62.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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