Pazopanib HCl

Synonyms: GW786034 HCl

Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.

Pazopanib HCl Chemical Structure

Pazopanib HCl Chemical Structure

CAS No. 635702-64-6

Purity & Quality Control

Pazopanib HCl Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 Function assay 14 to 24 hrs Inhibition of RIPK1 in human HT-29 cells assessed as reduction in TNFalpha-induced necroptosis incubated for 14 to 24 hrs in presence of Smac mimetic and z-VAD-FMK by cell titer glo-based luminescence assay, IC50=0.873μM 31622096
HT29 Antiproliferative assay Antiproliferative activity against human HT29 cells in serum containing medium 18620382
HN5 Antiproliferative assay Antiproliferative activity against human HN5 cells in serum containing medium 18620382
A375P Antiproliferative assay Antiproliferative activity against human A375P cells in serum containing medium 18620382
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
HUVEC Function assay 100 nM 2 hrs Inhibition of VEGF-stimulated VEGFR2 phosphorylation in human HUVEC cells at 100 nM preincubated for 2 hrs followed by VEGF stimulation by Western blot analysis 29787262
HUVEC Antiangiogenic assay 0.1 uM 6 hrs Antiangiogenic activity in human HUVEC cells assessed as reduction in capillary-like tubular network formation at 0.1 uM after 6 hrs by phase-contrast microscopy 29787262
MM Kinase assay inhibits VEGF-induced phosphorylation of flt1 17164332
MM.1S Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
MM.1R Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
RPMI Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
Dox40 Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
INA-6 Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
OPM2 Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
U266 Growth inhibitory assay 10 μg/mL inhibits MM Cell Growth 17164332
MM.1S cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
MM.1R cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
RPMI cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
Dox40 cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
INA-6 cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
OPM2 cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
U266 cytotoxicity assay 20 μg/mL inhibits MM Cell Survival 17164332
MM.1S Function assay suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. 17164332
MM.1R Function assay suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. 17164332
Dox40 Function assay suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. 17164332
OPM2 Function assay suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. 17164332
HBMEC Growth inhibitory assay ~10 μM DMSO IC50=1 μM 21081656
HBMEC Function assay ~1 μM DMSO abrogates the phosphorylation of VEGFR2 with disruption of downstream PLCγ1 21081656
HBMEC Function assay ~1 μM DMSO disrupts the Ras-Raf-ERK pathway through decreased phosphorylated MEK1/2 and ERK1/2 21081656
HBMEC Function assay ~20 μM DMSO disrupts 50% of tube formation at 1 μM 21081656
MDA-MB-231 Growth inhibitory assay ~10 μM DMSO IC50=5 μM 21081656
MDA-MB-231 Function assay 0.5 μM DMSO inhibits the ERK1/2 signaling pathway 21081656
MDA-MB-231 Function assay 5 μM DMSO induces a cell-cycle arrest 21081656
J82 cytotoxicity assay ~10 μM DMSO IC50=24.57 μM 21529900
T24 cytotoxicity assay ~10 μM DMSO IC50=52.45 μM 21529900
HT1376 cytotoxicity assay ~10 μM DMSO IC50=28.21 μM 21529900
RT4 cytotoxicity assay ~10 μM DMSO IC50=5.14 μM 21529900
CRL1749 cytotoxicity assay ~10 μM DMSO IC50=22.69 μM 21529900
HTB9 cytotoxicity assay ~10 μM DMSO IC50=11.84 μM 21529900
Sup cytotoxicity assay ~10 μM DMSO IC50=53.32 μM 21529900
HTB3 cytotoxicity assay ~10 μM DMSO IC50=14.16 μM 21529900
CEC Function assay ~10 μg/mL DMSO down-regulates VEGF levels 21620822
RPE Function assay ~10 μg/mL DMSO down-regulates VEGF levels 21620822
CEC Function assay ~5 μg/mL DMSO blocks endothelial cell migration 21620822
5637 Growth inhibitory assay DMSO IC50=15.0 μM 23887605
J82 Growth inhibitory assay DMSO IC50=18.4 μM 23887605
5637 Autophagy assay 20 μM DMSO triggers the autophagic process 23887605
J82 Autophagy assay 20 μM DMSO triggers the autophagic process 23887605
5637 Function assay 20 μM DMSO induces lysosomal-dependent necrosis 23887605
J82 Function assay 20 μM DMSO induces lysosomal-dependent necrosis 23887605
5637 Function assay 20 μM DMSO induces lysosome alteration and inhibits CB activity 23887605
J82 Function assay 20 μM DMSO induces lysosome alteration and inhibits CB activity 23887605
KATO-II Growth inhibitory assay 5 μM DMSO blocks proliferation 25249557
OCUM-2M Growth inhibitory assay 5 μM DMSO blocks proliferation 25249557
SNU-16 Growth inhibitory assay 5 μM DMSO blocks proliferation 25249557
HSC-39 Growth inhibitory assay 5 μM DMSO blocks proliferation 25249557
KATO-II cytotoxicity assay ~10 μM DMSO IC50=0.1 to 2.0 μmol/L 25249557
OCUM-2M cytotoxicity assay ~10 μM DMSO IC50=0.1 to 2.0 μmol/L 25249557
SNU-16 cytotoxicity assay ~10 μM DMSO IC50=0.1 to 2.0 μmol/L 25249557
HSC-39 cytotoxicity assay ~10 μM DMSO IC50=0.1 to 2.0 μmol/L 25249557
NIH 3T3 Growth inhibitory assay ~10 μM DMSO inhibits cell growth and colony formation 25249557
KATO-III Function assay 1 μM DMSO induces cell-cycle arrest 25249557
OCUM-2M Function assay 1 μM DMSO induces cell-cycle arrest 25249557
KATO-III Apoptosis assay 1 μM DMSO induces apoptosis 25249557
OCUM-2M Apoptosis assay 1 μM DMSO induces apoptosis 25249557
KATO-III Function assay 1 μM DMSO inhibits FGFR2 phosphorylation and downstream signaling molecules 25249557
EoL-1-cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000289μM. SANGER
AN3-CA Growth inhibition assay Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=0.01005μM. SANGER
CGTH-W-1 Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=0.04001μM. SANGER
GDM-1 Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.10399μM. SANGER
A204 Growth inhibition assay Inhibition of human A204 cell growth in a cell viability assay, IC50=0.10906μM. SANGER
G-402 Growth inhibition assay Inhibition of human G-402 cell growth in a cell viability assay, IC50=0.53184μM. SANGER
MFE-296 Growth inhibition assay Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=0.59022μM. SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.65987μM. SANGER
KG-1 Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=0.71755μM. SANGER
HT55 Growth inhibition assay Inhibition of human HT55 cell growth in a cell viability assay, IC50=0.98781μM. SANGER
MG-63 Growth inhibition assay Inhibition of human MG-63 cell growth in a cell viability assay, IC50=1.00146μM. SANGER
CCF-STTG1 Growth inhibition assay Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.04981μM. SANGER
RT-112 Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.10376μM. SANGER
MC-IXC Growth inhibition assay Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=1.11512μM. SANGER
HUTU-80 Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.28103μM. SANGER
MV-4-11 Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=1.34501μM. SANGER
LCLC-103H Growth inhibition assay Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=1.44549μM. SANGER
G-401 Growth inhibition assay Inhibition of human G-401 cell growth in a cell viability assay, IC50=1.46421μM. SANGER
A704 Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50=1.60323μM. SANGER
ESS-1 Growth inhibition assay Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=1.60396μM. SANGER
HLE Growth inhibition assay Inhibition of human HLE cell growth in a cell viability assay, IC50=1.63804μM. SANGER
NY Growth inhibition assay Inhibition of human NY cell growth in a cell viability assay, IC50=1.84821μM. SANGER
A427 Growth inhibition assay Inhibition of human A427 cell growth in a cell viability assay, IC50=1.98075μM. SANGER
SK-N-DZ Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=2.02381μM. SANGER
J82 Growth inhibition assay Inhibition of human J82 cell growth in a cell viability assay, IC50=2.06088μM. SANGER
GI-1 Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=2.22951μM. SANGER
NCI-H716 Growth inhibition assay Inhibition of human NCI-H716 cell growth in a cell viability assay, IC50=2.31633μM. SANGER
SF126 Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=2.47459μM. SANGER
H4 Growth inhibition assay Inhibition of human H4 cell growth in a cell viability assay, IC50=2.51262μM. SANGER
LB831-BLC Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=2.54566μM. SANGER
HCC1395 Growth inhibition assay Inhibition of human HCC1395 cell growth in a cell viability assay, IC50=2.58156μM. SANGER
LK-2 Growth inhibition assay Inhibition of human LK-2 cell growth in a cell viability assay, IC50=2.64569μM. SANGER
G-361 Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.04082μM. SANGER
NCI-H2342 Growth inhibition assay Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=3.13316μM. SANGER
SK-LU-1 Growth inhibition assay Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.18767μM. SANGER
IGROV-1 Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=3.24713μM. SANGER
EB2 Growth inhibition assay Inhibition of human EB2 cell growth in a cell viability assay, IC50=3.28168μM. SANGER
CAL-54 Growth inhibition assay Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=3.28367μM. SANGER
OCUB-M Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=3.31368μM. SANGER
LB1047-RCC Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=3.53164μM. SANGER
Daudi Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=3.66219μM. SANGER
A172 Growth inhibition assay Inhibition of human A172 cell growth in a cell viability assay, IC50=3.7379μM. SANGER
KGN Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=4.06709μM. SANGER
SNG-M Growth inhibition assay Inhibition of human SNG-M cell growth in a cell viability assay, IC50=4.08669μM. SANGER
SW1710 Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=4.47318μM. SANGER
Daoy Growth inhibition assay Inhibition of human Daoy cell growth in a cell viability assay, IC50=4.77949μM. SANGER
DMS-273 Growth inhibition assay Inhibition of human DMS-273 cell growth in a cell viability assay, IC50=4.96202μM. SANGER
KU812 Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=5.37812μM. SANGER
NCI-H727 Growth inhibition assay Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50=5.40901μM. SANGER
P30-OHK Growth inhibition assay Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=5.4694μM. SANGER
MIA-PaCa-2 Growth inhibition assay Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50=5.60466μM. SANGER
TT Growth inhibition assay Inhibition of human TT cell growth in a cell viability assay, IC50=5.6624μM. SANGER
DK-MG Growth inhibition assay Inhibition of human DK-MG cell growth in a cell viability assay, IC50=5.72028μM. SANGER
GB-1 Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay, IC50=5.73434μM. SANGER
NCI-H520 Growth inhibition assay Inhibition of human NCI-H520 cell growth in a cell viability assay, IC50=5.73435μM. SANGER
WM-115 Growth inhibition assay Inhibition of human WM-115 cell growth in a cell viability assay, IC50=5.75644μM. SANGER
CAL-72 Growth inhibition assay Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=5.9381μM. SANGER
NCI-H1573 Growth inhibition assay Inhibition of human NCI-H1573 cell growth in a cell viability assay, IC50=5.96542μM. SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=6.02688μM. SANGER
TE-8 Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=6.16473μM. SANGER
GAMG Growth inhibition assay Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.17776μM. SANGER
HGC-27 Growth inhibition assay Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=6.2015μM. SANGER
CTV-1 Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=6.20903μM. SANGER
NCI-H810 Growth inhibition assay Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=6.31365μM. SANGER
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=6.55237μM. SANGER
SNB75 Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=6.56939μM. SANGER
SK-MES-1 Growth inhibition assay Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=6.8663μM. SANGER
MZ2-MEL Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=6.93016μM. SANGER
TE-15 Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=7.16924μM. SANGER
S-117 Growth inhibition assay Inhibition of human S-117 cell growth in a cell viability assay, IC50=7.57924μM. SANGER
HuH-7 Growth inhibition assay Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=7.69384μM. SANGER
CAS-1 Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=7.76339μM. SANGER
D-502MG Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=7.78222μM. SANGER
IA-LM Growth inhibition assay Inhibition of human IA-LM cell growth in a cell viability assay, IC50=7.93364μM. SANGER
CAKI-1 Growth inhibition assay Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=8.28831μM. SANGER
KYSE-70 Growth inhibition assay Inhibition of human KYSE-70 cell growth in a cell viability assay, IC50=8.45447μM. SANGER
HCC1569 Growth inhibition assay Inhibition of human HCC1569 cell growth in a cell viability assay, IC50=8.46556μM. SANGER
SR Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=8.70202μM. SANGER
SH-4 Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=8.73653μM. SANGER
SW954 Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=8.75347μM. SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=8.7782μM. SANGER
IST-MEL1 Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=8.91086μM. SANGER
EFM-19 Growth inhibition assay Inhibition of human EFM-19 cell growth in a cell viability assay, IC50=8.92276μM. SANGER
KS-1 Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=8.97341μM. SANGER
786-0 Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=8.99139μM. SANGER
SK-OV-3 Growth inhibition assay Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.01236μM. SANGER
C3A Growth inhibition assay Inhibition of human C3A cell growth in a cell viability assay, IC50=9.12939μM. SANGER
NCI-H358 Growth inhibition assay Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50=9.15929μM. SANGER
NCI-H2170 Growth inhibition assay Inhibition of human NCI-H2170 cell growth in a cell viability assay, IC50=9.20801μM. SANGER
HMV-II Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=9.34065μM. SANGER
SW1088 Growth inhibition assay Inhibition of human SW1088 cell growth in a cell viability assay, IC50=9.56098μM. SANGER
RS4-11 Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=9.71841μM. SANGER
SNU-423 Growth inhibition assay Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=9.87712μM. SANGER
A431 Growth inhibition assay Inhibition of human A431 cell growth in a cell viability assay, IC50=9.88028μM. SANGER
BB65-RCC Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=10.0298μM. SANGER
M059J Growth inhibition assay Inhibition of human M059J cell growth in a cell viability assay, IC50=10.2576μM. SANGER
Calu-3 Growth inhibition assay Inhibition of human Calu-3 cell growth in a cell viability assay, IC50=10.5161μM. SANGER
LAMA-84 Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=10.6573μM. SANGER
ACHN Growth inhibition assay Inhibition of human ACHN cell growth in a cell viability assay, IC50=10.6743μM. SANGER
SW1990 Growth inhibition assay Inhibition of human SW1990 cell growth in a cell viability assay, IC50=10.7009μM. SANGER
LC-2-ad Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=10.7475μM. SANGER
U-698-M Growth inhibition assay Inhibition of human U-698-M cell growth in a cell viability assay, IC50=10.9926μM. SANGER
A2780 Growth inhibition assay Inhibition of human A2780 cell growth in a cell viability assay, IC50=11.0963μM. SANGER
VA-ES-BJ Growth inhibition assay Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=11.1909μM. SANGER
A253 Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay, IC50=11.3911μM. SANGER
NCI-H2087 Growth inhibition assay Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=11.7288μM. SANGER
NTERA-S-cl-D1 Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=11.7718μM. SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=11.8178μM. SANGER
LNCaP-Clone-FGC Growth inhibition assay Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=12.358μM. SANGER
HT-1376 Growth inhibition assay Inhibition of human HT-1376 cell growth in a cell viability assay, IC50=12.3595μM. SANGER
LB2518-MEL Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=12.4325μM. SANGER
QIMR-WIL Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=12.7363μM. SANGER
SF268 Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=12.9423μM. SANGER
MES-SA Growth inhibition assay Inhibition of human MES-SA cell growth in a cell viability assay, IC50=13.2346μM. SANGER
BPH-1 Growth inhibition assay Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=13.2694μM. SANGER
CA46 Growth inhibition assay Inhibition of human CA46 cell growth in a cell viability assay, IC50=13.3899μM. SANGER
LB373-MEL-D Growth inhibition assay Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=13.4353μM. SANGER
NCI-H1755 Growth inhibition assay Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=13.5203μM. SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=13.742μM. SANGER
SNU-387 Growth inhibition assay Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=13.9744μM. SANGER
HCC1419 Growth inhibition assay Inhibition of human HCC1419 cell growth in a cell viability assay, IC50=14.1325μM. SANGER
TE-9 Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=14.5343μM. SANGER
LCLC-97TM1 Growth inhibition assay Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=14.5912μM. SANGER
BC-1 Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=14.6038μM. SANGER
DU-145 Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=14.7605μM. SANGER
KARPAS-45 Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=15.1099μM. SANGER
SW684 Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50=15.1418μM. SANGER
HCC2218 Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=15.1714μM. SANGER
EW-13 Growth inhibition assay Inhibition of human EW-13 cell growth in a cell viability assay, IC50=15.8055μM. SANGER
D-392MG Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=15.8277μM. SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=15.8665μM. SANGER
Saos-2 Growth inhibition assay Inhibition of human Saos-2 cell growth in a cell viability assay, IC50=15.9353μM. SANGER
COLO-679 Growth inhibition assay Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=16.1233μM. SANGER
PC-14 Growth inhibition assay Inhibition of human PC-14 cell growth in a cell viability assay, IC50=16.4902μM. SANGER
CAL-85-1 Growth inhibition assay Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50=16.5837μM. SANGER
AU565 Growth inhibition assay Inhibition of human AU565 cell growth in a cell viability assay, IC50=16.7598μM. SANGER
A2058 Growth inhibition assay Inhibition of human A2058 cell growth in a cell viability assay, IC50=16.8504μM. SANGER
NH-12 Growth inhibition assay Inhibition of human NH-12 cell growth in a cell viability assay, IC50=17.5557μM. SANGER
Hs-578-T Growth inhibition assay Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=17.6584μM. SANGER
RXF393 Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=17.8039μM. SANGER
COLO-741 Growth inhibition assay Inhibition of human COLO-741 cell growth in a cell viability assay, IC50=18.1083μM. SANGER
NCI-H1355 Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=18.1318μM. SANGER
GI-ME-N Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=18.453μM. SANGER
MEL-HO Growth inhibition assay Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=18.9753μM. SANGER
SW982 Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay, IC50=19.8406μM. SANGER
MONO-MAC-6 Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=19.9061μM. SANGER
MFH-ino Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=20.2037μM. SANGER
BEN Growth inhibition assay Inhibition of human BEN cell growth in a cell viability assay, IC50=20.3128μM. SANGER
HT-144 Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=20.3697μM. SANGER
DoTc2-4510 Growth inhibition assay Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50=20.7966μM. SANGER
NCI-H522 Growth inhibition assay Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50=20.8971μM. SANGER
NCI-H1299 Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=21.167μM. SANGER
CAL-12T Growth inhibition assay Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=21.2435μM. SANGER
CTB-1 Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=21.6855μM. SANGER
COR-L105 Growth inhibition assay Inhibition of human COR-L105 cell growth in a cell viability assay, IC50=21.7949μM. SANGER
NCI-H1650 Growth inhibition assay Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50=21.8133μM. SANGER
SK-MEL-3 Growth inhibition assay Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=21.9788μM. SANGER
697 Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=22.0402μM. SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50=22.1998μM. SANGER
ACN Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=22.4965μM. SANGER
MHH-PREB-1 Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=22.5088μM. SANGER
RPMI-6666 Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=22.5905μM. SANGER
BB30-HNC Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=23.539μM. SANGER
HOS Growth inhibition assay Inhibition of human HOS cell growth in a cell viability assay, IC50=23.8014μM. SANGER
OVCAR-4 Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=23.984μM. SANGER
SK-HEP-1 Growth inhibition assay Inhibition of human SK-HEP-1 cell growth in a cell viability assay, IC50=24.0791μM. SANGER
OS-RC-2 Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=24.0858μM. SANGER
MKN1 Growth inhibition assay Inhibition of human MKN1 cell growth in a cell viability assay, IC50=24.1401μM. SANGER
NCI-H510A Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=24.5517μM. SANGER
DBTRG-05MG Growth inhibition assay Inhibition of human DBTRG-05MG cell growth in a cell viability assay, IC50=25.014μM. SANGER
SW13 Growth inhibition assay Inhibition of human SW13 cell growth in a cell viability assay, IC50=25.0254μM. SANGER
HuO-3N1 Growth inhibition assay Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=25.2535μM. SANGER
U-2-OS Growth inhibition assay Inhibition of human U-2-OS cell growth in a cell viability assay, IC50=25.5982μM. SANGER
PANC-10-05 Growth inhibition assay Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50=25.8389μM. SANGER
NUGC-3 Growth inhibition assay Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50=26.0051μM. SANGER
MZ1-PC Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=26.2821μM. SANGER
U-118-MG Growth inhibition assay Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=26.3272μM. SANGER
NCI-H1703 Growth inhibition assay Inhibition of human NCI-H1703 cell growth in a cell viability assay, IC50=26.4593μM. SANGER
HT-1080 Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=26.6211μM. SANGER
EFO-21 Growth inhibition assay Inhibition of human EFO-21 cell growth in a cell viability assay, IC50=26.7536μM. SANGER
TK10 Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay, IC50=27.1653μM. SANGER
ES1 Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=27.6673μM. SANGER
DMS-153 Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=28.2498μM. SANGER
KYSE-270 Growth inhibition assay Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=28.3533μM. SANGER
MLMA Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50=28.3719μM. SANGER
KURAMOCHI Growth inhibition assay Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=28.5975μM. SANGER
NCI-H2347 Growth inhibition assay Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50=28.5994μM. SANGER
MCF7 Growth inhibition assay Inhibition of human MCF7 cell growth in a cell viability assay, IC50=28.7093μM. SANGER
HOP-92 Growth inhibition assay Inhibition of human HOP-92 cell growth in a cell viability assay, IC50=28.9327μM. SANGER
REH Growth inhibition assay Inhibition of human REH cell growth in a cell viability assay, IC50=28.9422μM. SANGER
RT4 Growth inhibition assay Inhibition of human RT4 cell growth in a cell viability assay, IC50=29.2259μM. SANGER
HT-1197 Growth inhibition assay Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=29.2582μM. SANGER
BL-41 Growth inhibition assay Inhibition of human BL-41 cell growth in a cell viability assay, IC50=29.6923μM. SANGER
IST-MES1 Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=29.8144μM. SANGER
MOLT-16 Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=30.3744μM. SANGER
GAK Growth inhibition assay Inhibition of human GAK cell growth in a cell viability assay, IC50=31.1007μM. SANGER
RD Growth inhibition assay Inhibition of human RD cell growth in a cell viability assay, IC50=31.2473μM. SANGER
COR-L23 Growth inhibition assay Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=31.3023μM. SANGER
Capan-2 Growth inhibition assay Inhibition of human Capan-2 cell growth in a cell viability assay, IC50=31.6669μM. SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=31.9592μM. SANGER
BCPAP Growth inhibition assay Inhibition of human BCPAP cell growth in a cell viability assay, IC50=32.4534μM. SANGER
OVCAR-3 Growth inhibition assay Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=32.6497μM. SANGER
NKM-1 Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=33.1404μM. SANGER
647-V Growth inhibition assay Inhibition of human 647-V cell growth in a cell viability assay, IC50=33.9321μM. SANGER
ES5 Growth inhibition assay Inhibition of human ES5 cell growth in a cell viability assay, IC50=34.9282μM. SANGER
A3-KAW Growth inhibition assay Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=35.5285μM. SANGER
ChaGo-K-1 Growth inhibition assay Inhibition of human ChaGo-K-1 cell growth in a cell viability assay, IC50=35.5964μM. SANGER
NALM-6 Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=35.6045μM. SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=35.9586μM. SANGER
BL-70 Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=36.8348μM. SANGER
MRK-nu-1 Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=37.0227μM. SANGER
COR-L88 Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=37.2976μM. SANGER
MDA-MB-415 Growth inhibition assay Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=38.6783μM. SANGER
Becker Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=39.1235μM. SANGER
NCI-H2452 Growth inhibition assay Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=39.1445μM. SANGER
SW626 Growth inhibition assay Inhibition of human SW626 cell growth in a cell viability assay, IC50=39.1841μM. SANGER
SAS Growth inhibition assay Inhibition of human SAS cell growth in a cell viability assay, IC50=39.5476μM. SANGER
DMS-53 Growth inhibition assay Inhibition of human DMS-53 cell growth in a cell viability assay, IC50=39.7553μM. SANGER
CP66-MEL Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=39.7602μM. SANGER
NCI-H2405 Growth inhibition assay Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50=40.1926μM. SANGER
MC-CAR Growth inhibition assay Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=40.2471μM. SANGER
CAL-120 Growth inhibition assay Inhibition of human CAL-120 cell growth in a cell viability assay, IC50=40.9723μM. SANGER
GCT Growth inhibition assay Inhibition of human GCT cell growth in a cell viability assay, IC50=41.2626μM. SANGER
A375 Growth inhibition assay Inhibition of human A375 cell growth in a cell viability assay, IC50=41.5395μM. SANGER
MEG-01 Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=41.6116μM. SANGER
NCI-H2122 Growth inhibition assay Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=41.97μM. SANGER
RPMI-2650 Growth inhibition assay Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=43.4784μM. SANGER
8305C Growth inhibition assay Inhibition of human 8305C cell growth in a cell viability assay, IC50=43.7675μM. SANGER
NCI-H1395 Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=44.1055μM. SANGER
EW-16 Growth inhibition assay Inhibition of human EW-16 cell growth in a cell viability assay, IC50=44.1094μM. SANGER
T98G Growth inhibition assay Inhibition of human T98G cell growth in a cell viability assay, IC50=44.4245μM. SANGER
IST-SL2 Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=44.9279μM. SANGER
NCI-H1651 Growth inhibition assay Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=45.9208μM. SANGER
COR-L279 Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=46.2081μM. SANGER
YT Growth inhibition assay Inhibition of human YT cell growth in a cell viability assay, IC50=46.5067μM. SANGER
TE-11 Growth inhibition assay Inhibition of human TE-11 cell growth in a cell viability assay, IC50=46.7404μM. SANGER
C-33-A Growth inhibition assay Inhibition of human C-33-A cell growth in a cell viability assay, IC50=46.8197μM. SANGER
OVCAR-5 Growth inhibition assay Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50=47.2307μM. SANGER
PANC-03-27 Growth inhibition assay Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=47.3513μM. SANGER
CaR-1 Growth inhibition assay Inhibition of human CaR-1 cell growth in a cell viability assay, IC50=48.2474μM. SANGER
SNU-449 Growth inhibition assay Inhibition of human SNU-449 cell growth in a cell viability assay, IC50=49.2285μM. SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
Features A multi-kinase inhibitor.
Targets
VEGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
FGFR [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
Click to View More Targets
10 nM 30 nM 47 nM 74 nM 84 nM
In vitro
In vitro Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. [1] Pazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of Pazopanib and is completely abolished at 5 µg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. [2] Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. [3]
Kinase Assay Kinase enzyme assays
VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated Pazopanib in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs.
Cell Research Cell lines HUVEC cells
Concentrations 0-10 μM
Incubation Time 1 hour
Method

Phosphorylation of VEGFR2 is assessed in HUVEC stimulated with VEGF. HUVEC are plated in type-I collagen-coated 10 cm plates in Clonetics EGM-MV medium at 1.0-1.5 × 106 cells/plate. After 24 hours, the confluent cells are serum starved overnight by replacing the growth medium with Clonetics EBM medium containing 0.1% BSA, 500 μg/mL hydrocortisone. Cells are treated with Pazopanib at various concentrations for 1 hour, followed by addition of 10 ng/mL VEGF or vehicle for 10 min. Cells are solubilized in lysis buffer. VEGFR2 is immunoprecipitated using antiflk-1 antibody and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Western blotting and detection with antiflk-1 or with antiphosphotyrosine (anti-P-tyr-biotin) antibody. The VEGFR2 phosphorylation level is quantified by densitometry and normalized to the total VEGFR2 level.

Experimental Result Images Methods Biomarkers Images PMID
Western blot p53 / PUMA p-Akt / Akt p-VEGFR2 / p-c-Kit / p-PDGFRβ / FLT-3 27924057
Immunofluorescence YAP/TAZ 26199863
Growth inhibition assay Cell viability 27924057
In Vivo
In vivo The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group. [2]
Animal Research Animal Models Immunodeficient mice bearing SYO-1 cells
Dosages 0 mg/kg, 10 mg/kg, 30 mg/kg, or 100 mg/kg
Administration Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03850964 Recruiting
Hereditary Hemorrhagic Telangiectasia|Epistaxis|Anemia|Nosebleed|HHT
Cure HHT
May 8 2023 Phase 2|Phase 3
NCT05180695 Recruiting
Advanced Soft-tissue Sarcoma|Metastatic Soft-tissue Sarcoma
Centre Leon Berard|Novartis|National Cancer Institute France
April 15 2022 Phase 1|Phase 2
NCT03735758 Terminated
Soft Tissue Sarcoma Adult
GWT-TUD GmbH
November 2 2018 Phase 4

Chemical Information & Solubility

Molecular Weight 473.98 Formula

C21H23N7O2S.HCl

CAS No. 635702-64-6 SDF Download Pazopanib HCl SDF
Smiles CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (200.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 95 mg/mL

Ethanol : 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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