Home Protein Tyrosine Kinase EGFR inhibitor - Autophagy activator Erlotinib HCl For research use only.

Erlotinib HCl

Synonyms: CP358774, NSC 718781,OSI-774 HCl

Erlotinib HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Erlotinib HCl Chemical Structure

Erlotinib HCl Chemical Structure

CAS No. 183319-69-9

Purity & Quality Control

Erlotinib HCl Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SKBR3 cells Function assay Inhibition of HER2 in human SKBR3 cells by HTRF assay, IC50=1.89 μM. 19815412
human A431 cells Function assay Inhibition of EGFR in human A431 cells by HTRF assay, IC50=0.42 μM. 19815412
A431 Function assay Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA assay, IC50 = 0.0012 μM. 24890652
MCF7 Cytotoxicity assay Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0012 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 = 0.0012 μM. 30098869
A431 Function assay 60 mins Inhibition of EGFR in human A431 cells assessed as reduction in EGF induced phosphorylation preincubated for 60 mins followed by EGF addition measured after 10 mins by ELISA method, IC50 = 0.0012 μM. 27894589
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 = 0.0012 μM. 25882519
HCC827 Cytotoxicity assay 48 hrs Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay, IC50 = 0.002 μM. 24900830
PC9 Function assay 2 hrs Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50 = 0.0059 μM. 23930994
NCI-H292 Function assay 1 hr Inhibition of EGFR phosphorylation in human NCI-H292 cells preincubated for 1 hr followed by stimulation with EGF for 8 mins by electrochemiluminescent immunoassay, IC50 = 0.0063 μM. 26455919
HCC827 Function assay 2 hrs Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA, IC50 = 0.008 μM. 26756222
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.01 μM. 19914837
H3255 Function assay 2 hrs Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA, IC50 = 0.01 μM. 26756222
H3255 Function assay 2 hrs Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 0.01 μM. 28287730
PC9 Function assay 2 hrs Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA, IC50 = 0.011 μM. 26756222
A549 Function assay 2 hrs Inhibition of EGF-stimulated wild-type EGFR phosphorylation in human A549 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 0.011 μM. 28287730
PC9 Function assay 2 hrs Inhibition of EGFR exon 19 deletion mutant phosphorylation in human PC9 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 0.011 μM. 28287730
A549 Function assay Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50 = 0.011 μM. 26756222
BA/F3 Cytotoxicity assay Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant, IC50 = 0.0125 μM. 19239229
KB Function assay 1 hr Inhibition of EGF-stimulated autophosphorylation of EGFR in human KB cells incubated for 1 hr prior to EGF challenge measured after 6 mins by ELISA, IC50 = 0.019 μM. 24411123
NIH3T3 Function assay Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells, IC50 = 0.0193 μM. 16480284
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 19914835
Sf9 Function assay Inhibition of cloned EGFR autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.02 μM. 19914837
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 20005116
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 20594859
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 22277588
A16-F10 Antiproliferative assay 48 hrs Antiproliferative activity against human A16-F10 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 22112541
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 21802290
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 20627597
HT-29 Antiproliferative assay 48 hrs Antiproliferative activity human HT-29 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.02 μM. 29407956
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 23245802
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells after 72 hrs by CCK-8 assay, IC50 = 0.029 μM. 26487917
Sf9 Function assay Inhibition of cloned EGFR autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.03 μM. 19914835
Sf9 Function assay 1 hr Inhibition of human recombinant His6x-tagged EGFR autophosphorylation expressed in Sf9 cells after 1 hr by ELISA, IC50 = 0.03 μM. 20594859
Sf9 Function assay 1 hr Inhibition of autophosphorylation of recombinant His-tagged EGFR expressed in baculovirus infected Sf9 cells after 1 hr by DELFIA/time-resolved fluorimetry assay, IC50 = 0.03 μM. 22277588
Sf9 Function assay 10 mins Inhibition of EGFR expressed in baculovirus infected Sf9 cells assessed as inhibition of autophosphorylation preincubated for 10 mins measured after 1 hr by DELFIA/Time-Resolved Fluorometry, IC50 = 0.03 μM. 22112541
Sf9 Function assay 1 hr Inhibition of histidine-tagged human recombinant cytoplasmic domain of EGFR expressed in baculovirus infected insect Sf9 cells after 1 hr by DELFIA/time-resolved fluorometric analysis, IC50 = 0.03 μM. 22361272
Sf9 Function assay 1 hr Inhibition of recombinant EGFR expressed in baculovirus infected Sf9 cells after 1 hr by DELFIA/time-resolved fluorimetry assay, IC50 = 0.03 μM. 21763148
Sf9 Function assay 1 hr Inhibition of His-tagged EGFR expressed in insect Sf9 cells after 1 hr by time-resolved fluorimetric analysis, IC50 = 0.03 μM. 21816517
Sf9 Function assay Inhibition of histidine-tagged recombinant EGFR autophosphorylation expressed in Sf9 cells by solid-phase ELISA, IC50 = 0.03 μM. 20627597
MIAPaCa2 Antiproliferative assay 48 hrs Antiproliferative activity human MIAPaCa2 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.03 μM. 29407956
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity human MCF7 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.03 μM. 29407956
PC3 Antiproliferative assay 48 hrs Antiproliferative activity human PC3 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.03 μM. 29407956
Sf9 Function assay Inhibition of histidine-tagged recombinant EGFR cytoplasmic domain (amino acids 645-1186) (unknown origin) expressed in Sf9 cells assessed as reduction in enzyme autophosphorylation by DELFIA/time-resolved fluorometry, IC50 = 0.03 μM. 25172421
Sf9 Function assay Inhibition of EGFR cytoplasmic domain (amino acids 645 to 1186) (unknown origin) expressed in Sf9 cells assessed as reduction in enzyme autophosphorylation by DELFIA time resolved fluorometry, IC50 = 0.03 μM. 23245570
A549 Antiproliferative assay 24 hrs Antiproliferative activity against human A549 cells after 24 hrs by MTT assay, GI50 = 0.03 μM. 23391364
Sf9 Function assay 10 mins Inhibition of recombinant EGFR kinase cytoplasmic domain (unknown origin) expressed in baculovirus expression vector-infected insect sf9 cells assessed as level of autophosphorylation after 10 mins by DELFIA/time-resolved fluorometry, IC50 = 0.03 μM. 23962660
NCI-H292 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR after 72 hrs by luminescence assay, EC50 = 0.031 μM. 26455919
Sf9 Function assay 1 hr Inhibition of autophosphorylation of recombinant EGFR cytoplasmic domain (645 to 1186) (unknown origin) expressed in Sf9 cells after 1 hr by DELFIA/time-resolved fluorometric analysis, IC50 = 0.032 μM. 24607998
Sf9 Function assay 1 hr Inhibition of autophosphorylation of EGFR cytoplasmic domain (amino acids 645 to 1186) (unknown origin) expressed in Sf9 cells after 1 hr by time-resolved fluorometry, IC50 = 0.032 μM. 24630412
Sf9 Function assay 10 mins Inhibition of recombinant EGFR cytoplasmic domain (645 to 1186) (unknown origin) autophosphorylation expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by ATP-MgCl2 addition measured after 1 hr by fluorometric analysis, IC50 = 0.032 μM. 24144854
A431 Function assay Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.034 μM. 20346655
A549 Antiproliferative assay 48 hrs Antiproliferative activity human A549 cells after 48 hrs by propidium iodide staining-based fluorescence assay, IC50 = 0.04 μM. 29407956
B16/F10 Antiproliferative assay 48 hrs Antiproliferative activity against mouse B16/F10 cells after 48 hrs by MTT assay, IC50 = 0.05 μM. 23245802
MIAPaCa Function assay Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.051 μM. 20817523
A431 Cytotoxicity assay 48 hrs Cytotoxicity against human A431 cells over expressing EGFR after 48 hrs by MTT assay, IC50 = 0.055 μM. 22414612
Sf9 Function assay Inhibition of recombinant full-length GST-tagged human B-RAF V600E mutant (417 to 766 residues) expressed in Baculovirus infected Sf9 cells using N-terminal His-tagged human MEK1 as substrate by Nu-page gel-based phosphor screen analysis, IC50 = 0.06 μM. 29549841
Sf9 Function assay 10 mins Inhibition of His6-tagged recombinant EGFR cytoplasmic domain (unknown origin) (645 to 1186 residues) expressed in baculovirus infected Sf-9 cells preincubated for 10 mins followed by ATP addition measured after 1 hr by DELFIA/Time-Resolved fluorometry, IC50 = 0.06 μM. 28431353
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.07 μM. 22361272
PC9 Antiproliferative assay 96 hrs Antiproliferative activity against human PC9 cells after 96 hrs by Sytox green marker based fluorescence analysis, IC50 = 0.07 μM. 26599532
LoVo Function assay 2 hrs Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay, IC50 = 0.077 μM. 23930994
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.08 μM. 21816517
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.08 μM. 28988624
Sf9 Function assay 10 mins Inhibition of His6-tagged EGFR (unknown origin) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells after 10 mins followed by addition of ATP-MgCl2 and measured after 1 hr by time-resolved fluorometric analysis, IC50 = 0.08 μM. 29407956
Sf9 Function assay Inhibition of His-6 tagged recombinant EGFR cytoplasmic domain (645 to 1186 residues) (unknown origin) expressed in Baculovirus infected Sf9 cells by dissociation-enhanced lanthanide fluorescence immunoassay/time-resolved fluorometric analysis, IC50 = 0.08 μM. 29549841
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, GI50 = 0.08 μM. 23391364
BA/F3 Function assay 48 hrs Inhibition of EGFR L858R mutant (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by XTT assay, IC50 = 0.087 μM. 27235841
Sf9 Function assay 5 mins Inhibition of recombinant human GST-tagged HER2 (676-end) expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.091 μM. 30096580
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.096 μM. 19888761
B16F10 Antiproliferative assay 48 hrs Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 22361272
MCF7 Antiproliferative assay 12 hrs Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.1 μM. 26652482
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 25172421
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 25172421
Sf9 Function assay Inhibition of human cloned HER2 autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.12 μM. 19914837
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. 22112541
B16F10 Antiproliferative assay 48 hrs Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. 28988624
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. 24607998
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. 24630412
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.12 μM. 24144854
HepG2 Antiproliferative assay 12 hrs Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.12 μM. 26652482
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. 23245570
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 0.12 μM. 23962660
U251 Function assay Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay, IC50 = 0.1247 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 = 0.1247 μM. 30098869
U251 Function assay 60 mins Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.1247 μM. 25882519
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.13 μM. 24607998
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.13 μM. 24630412
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.13 μM. 24144854
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.13 μM. 23962660
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 0.14 μM. 22361272
DIFI Cytotoxicity assay 4 days Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.14 μM. 22169601
Sf9 Function assay 1 hr Inhibition of histidine-tagged human recombinant cytoplasmic domain of HER2 expressed in baculovirus infected insect Sf9 cells after 1 hr by DELFIA/time-resolved fluorometric analysis, IC50 = 0.14 μM. 22361272
Sf9 Function assay Inhibition of human cloned HER2 autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA, IC50 = 0.16 μM. 19914835
Sf9 Function assay 1 hr Inhibition of human recombinant His6x-tagged HER2 autophosphorylation expressed in Sf9 cells after 1 hr by ELISA, IC50 = 0.16 μM. 20594859
Sf9 Function assay 1 hr Inhibition of autophosphorylation of human HER2 cytoplasmic domain (amino acids 676 to 1245) (unknown origin) expressed in Sf9 cells after 1 hr by time-resolved fluorometry, IC50 = 0.16 μM. 24630412
Sf9 Function assay Inhibition of human HER2 cytoplasmic domain (amino acids 676 to 1245) expressed in Sf9 cells by DELFIA time resolved fluorometry, IC50 = 0.16 μM. 23245802
B16F10 Antiproliferative assay 12 hrs Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.17 μM. 26652482
HeLa Antiproliferative assay 12 hrs Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.2 μM. 26652482
Sf9 Function assay Inhibition of histidine-tagged recombinant HER2 (unknown origin) expressed in Sf9 cells assessed as reduction in enzyme autophosphorylation by DELFIA/time-resolved fluorometry, IC50 = 0.2 μM. 25172421
A16-F10 Antiproliferative assay 48 hrs Antiproliferative activity against human A16-F10 cells after 48 hrs by MTT assay, IC50 = 0.2 μM. 23245570
MDA-MB-468 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.2352 μM. 24890652
CAL27 Cytotoxicity assay 4 days Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.239 μM. 22169601
Sf9 Function assay 5 mins Inhibition of GST-tagged recombinant human VEGFR (789-end) expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.25 μM. 30096580
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells expressing EGFR assessed as inhibition of basal cell growth after 48 hrs by MTT assay, IC50 = 0.27 μM. 21763148
T24 NIH Function assay Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells, IC50 = 0.299 μM. 16480284
GXF251L Cytotoxicity assay 4 days Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.369 μM. 22169601
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.409 μM. 24183742
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.4385 μM. 24890652
A431 Growth inhibition assay 72 hrs Growth inhibition of human A431 cells overexpressing EGFR after 72 hrs by MTT assay, GI50 = 0.47 μM. 17983745
BA/F3 Growth inhibition assay 96 hrs Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. 20222733
BA/F3 Growth inhibition assay 96 hrs Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. 20222733
BA/F3 Growth inhibition assay 96 hrs Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. 20222733
BA/F3 Growth inhibition assay 96 hrs Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay, GI50 = 0.5 μM. 20222733
Huh7.5 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus J6/JFH infected in human Huh7.5 cells assessed as inhibition of viral replication measured after 72 hrs by luciferase reporter gene assay, EC50 = 0.5 μM. 25822739
Huh7.5 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus J6/JFH electroporated in human Huh7.5 cells assessed as inhibition of intracellular infectivity drug treated every 24 hrs for 72 hrs measured 72 hrs post electroporation by luciferase reporter gene assay, EC50 = 0.5 μM. 25822739
Huh7.5 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus J6/JFH infected in human Huh7.5 cells assessed as inhibition of extracellular infectivity drug treated every 24 hrs for 72 hrs measured after 72 hrs by luciferase reporter gene assay, EC50 = 0.5 μM. 25822739
HEK293 Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki = 0.53 μM. 22541068
HEK293 Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50 = 0.55 μM. 22541068
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.56 μM. 24565969
MDA-MB-435 Cytotoxicity assay Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.6221 μM. 24890652
LXFA 629L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.66 μM. 22169601
A549 Cytotoxicity assay 24 hrs Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50 = 0.73 μM. 29028534
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells expressing EGFR after 72 hrs by MTT assay, IC50 = 0.75 μM. 24411123
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells after 72 hrs by CCK-8 assay, IC50 = 0.844 μM. 26487917
A431 Growth inhibition assay 72 hrs Growth inhibition of human A431 cells after 72 hrs by MTT assay, GI50 = 0.915 μM. 19969465
Calu3 Cytotoxicity assay 72 hrs Cytotoxicity against human Calu3 cells expressing HER2 after 72 hrs by MTT assay, IC50 = 0.93 μM. 24411123
DU145 Cytotoxicity assay 4 days Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.966 μM. 22169601
NCI-H2122 Antiproliferative assay Antiproliferative activity against human NCI-H2122 cells, IC50 = 1 μM. 20143778
NCI-H292 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H292 cells after 72 hrs by SRB assay, IC50 = 1 μM. 25215856
A431 Function assay 10 mins Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA, IC50 = 1.2 μM. 20403700
A431 Function assay Inhibition of EGFR expressed in human A431 cells, IC50 = 1.2 μM. 20558072
A431 Function assay 60 mins Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA, IC50 = 1.2 μM. 22204741
A431 Function assay 60 mins Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 1.2 μM. 23375090
A431 Function assay 60 mins Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA, IC50 = 1.2 μM. 23434139
A431 Function assay 60 mins Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 1.2 μM. 22739090
H9 Antiproliferative assay 72 hrs Antiproliferative activity against human H9 cells after 72 hrs by CellTiter-Glo assay, IC50 = 1.3 μM. 26599532
PC9 Function assay 24 hrs Inhibition of EGFR phosphorylation in human PC9 cells after 24 hrs by by Western blot analysis, IC50 = 1.36 μM. 22980218
SK-BR-3 Antiproliferative assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 1.56 μM. 20143778
LXFA 289L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.78 μM. 22169601
SCC15 Antiproliferative assay Antiproliferative activity against human SCC15 cells, IC50 = 1.94 μM. 20143778
Jurkat Growth inhibition assay 24 hrs Growth inhibition of human Jurkat cells after 24 hrs, IC50 = 2 μM. 17178722
erythroleukemia cell Growth inhibition assay 24 hrs Growth inhibition of JAK2 V617F mutant expressing human erythroleukemia cells after 24 hrs, IC50 = 2 μM. 17178722
erythroleukemia cell Growth inhibition assay 24 hrs Growth inhibition of mouse erythroleukemia cells after 24 hrs, IC50 = 2 μM. 17178722
NCI-H1993 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay, IC50 = 2.043 μM. 24900830
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay, IC50 = 2.98 μM. 25468044
PANC1 Growth inhibition assay 72 hrs Growth inhibition of human PANC1 cells after 72 hrs by CCK-8 assay, IC50 = 3.1 μM. 26547690
SCC25 Antiproliferative assay Antiproliferative activity against human SCC25 cells, IC50 = 3.34 μM. 20143778
NCI-H358 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 48 hrs by cck8 assay, IC50 = 3.91 μM. 27234887
COS7 Function assay Inhibition of human JAK2 V617F mutant expressed in COS7 cells, IC50 = 4 μM. 17178722
L3.6PL Growth inhibition assay 72 hrs Growth inhibition of human L3.6PL cells after 72 hrs by CCK-8 assay, IC50 = 4 μM. 26547690
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay, IC50 = 4.37 μM. 25468044
OVCAR3 Antiproliferative assay 72 hrs Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter-Glo assay, IC50 = 4.6 μM. 26599532
Calu3 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu3 cells after 72 hrs by CellTiter blue assay, IC50 = 4.7 μM. 26599532
hematopoietic progenitor cell Growth inhibition assay Growth inhibition of JAK2 V617F mutant expressing hematopoietic progenitor cells isolated from polycythemia vera patient by colony forming assay, IC50 = 5 μM. 17178722
KB Antiproliferative assay 48 hrs Antiproliferative activity against human KB cells expressing EGFR and Src after 48 hrs by SRB assay, IC50 = 5 μM. 26188620
N87 Function assay Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 5.2 μM. 20346655
NCI-H1975 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50 = 5.51 μM. 24411123
MRC5 Antiproliferative assay 72 hrs Antiproliferative activity against human MRC5 cells after 72 hrs by CellTiter-Glo assay, IC50 = 5.8 μM. 26599532
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 5.8 μM. 26896708
NCI-H358 Antiproliferative assay Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay, IC50 = 6 μM. 20143778
A549 Antiproliferative assay Antiproliferative activity against human A549 cells assessed as viable cells after 48 hrs by CCK8 assay, IC50 = 6.26 μM. 26879314
LNCAP Cytotoxicity assay 4 days Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.63 μM. 22169601
MIAPaCa Function assay Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 6.73 μM. 20817523
NCI-H358 Antiproliferative assay Antiproliferative activity against human NCI-H358 cells assessed as viable cells after 48 hrs by CCK8 assay, IC50 = 6.85 μM. 26879314
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant after 72 hrs by SRB assay, IC50 = 6.9 μM. 24183742
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 7.06 μM. 24565969
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 7.099 μM. 24900830
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by cck8 assay, IC50 = 7.35 μM. 27234887
NCI-H1975 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay, IC50 = 7.498 μM. 24900830
HCC827 Antiproliferative assay Antiproliferative activity against human HCC827 cells after hrs by ATP content assay, IC50 = 7.5 μM. 20143778
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay, IC50 = 7.59 μM. 25468044
BxPC3 Antiproliferative assay Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay, IC50 = 7.6 μM. 20143778
NCI-H1975 Function assay 2 hrs Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50 = 7.6 μM. 23930994
PCI35 Growth inhibition assay 72 hrs Growth inhibition of human PCI35 cells after 72 hrs by CCK-8 assay, IC50 = 7.7 μM. 26547690
WM266.4 Antiproliferative assay 24 hrs Antiproliferative activity against human WM266.4 cells after 24 hrs by MTT assay, IC50 = 8.09 μM. 22985957
WM266.4 Growth inhibition assay 24 hrs Growth inhibition in human WM266.4 cells after 24 hrs by MTT reduction assay, GI50 = 8.12 μM. 22985962
WM266.4 Antiproliferative assay 24 hrs Antiproliferative activity against human WM266.4 cells assessed as cell viability after 24 hrs by MTT assay, GI50 = 8.14 μM. 27238841
H460 Antiproliferative assay Antiproliferative activity against human H460 cells after hrs by ATP content assay, IC50 = 8.2 μM. 20143778
OVXF 899L Cytotoxicity assay 4 days Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.77 μM. 22169601
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 8.97 μM. 22985957
NCI-H1975 Function assay 2 hrs Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA, IC50 = 9 μM. 26756222
H1975 Function assay 2 hrs Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 9.003 μM. 28287730
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay, IC50 = 9.1 μM. 25468044
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by SRB assay, IC50 = 9.5 μM. 25215856
PC9-DRH Function assay 2 hrs Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA, IC50 = 9.7 μM. 26756222
PC9-DRH Function assay 2 hrs Inhibition of EGFR T790M/exon 19 deletion mutant phosphorylation in human PC9-DRH cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA, IC50 = 9.736 μM. 28287730
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells after 72 hrs by CellTiter blue assay, IC50 = 9.9 μM. 26599532
PAXF 546L Cytotoxicity assay 4 days Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10 μM. 22169601
RXF 486L Cytotoxicity assay 4 days Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10 μM. 22169601
CAL27 Antiproliferative assay Antiproliferative activity against human CAL27 cells, IC50 = 10.15 μM. 20143778
SKHEP1 Antiproliferative assay Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 10.37 μM. 20143778
MDA-MB-468 Antiproliferative assay Antiproliferative activity against human MDA-MB-468 cells, IC50 = 11.4 μM. 20143778
SF539 Function assay 60 mins Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 12.2 μM. 23375090
SF539 Function assay 60 mins Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA, IC50 = 12.2 μM. 23434139
SF539 Function assay 60 mins Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 12.2 μM. 22739090
A498 Antiproliferative assay 48 hrs Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 12.5 μM. 29057042
NCI-H661 Cytotoxicity assay 4 to 5 days Cytotoxicity against human NCI-H661 cells after 4 to 5 days by MTT assay, IC50 = 12.71 μM. 20466555
BT474 Antiproliferative assay 72 hrs Antiproliferative activity against human BT474 cells after 72 hrs by CellTiter blue assay, IC50 = 13 μM. 26599532
BXF T24 Cytotoxicity assay 4 days Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.9 μM. 22169601
CXF 269L Cytotoxicity assay 4 days Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 16 μM. 22169601
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 = 16.2 μM. 28230985
PC3M Cytotoxicity assay 4 days Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 17.2 μM. 22169601
A549 Anticancer assay 96 hrs Anticancer activity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay, IC50 = 17.32 μM. 29549841
LXFL 529L Cytotoxicity assay 4 days Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 17.4 μM. 22169601
FADU Antiproliferative assay Antiproliferative activity against human FADU cells, IC50 = 18 μM. 26599532
LNCAP Antiproliferative assay Antiproliferative activity against human LNCAP cells, IC50 = 18.35 μM. 20143778
LO2 Cytotoxicity assay 48 hrs Cytotoxicity against human LO2 cells after 48 hrs by MTT assay, IC50 = 18.5 μM. 26896708
MEXF 276L Cytotoxicity assay 4 days Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 18.6 μM. 22169601
DU145 Cytotoxicity assay 4 to 5 days Cytotoxicity against human DU145 cells after 4 to 5 days by MTT assay, IC50 = 19.4 μM. 20466555
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 20 μM. 30047410
Saos2 Cytotoxicity assay 4 days Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 21 μM. 22169601
HEK293 Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50 = 21 μM. 22541068
HEK293 Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki = 21 μM. 22541068
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 21.3 μM. 28886509
H460/Vbl Cytotoxicity assay 72 hrs Cytotoxicity against human H460/Vbl cells after 72 hrs by SRB assay, IC50 = 21.5 μM. 25215856
UXF 1138L Cytotoxicity assay 4 days Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 24.5 μM. 22169601
MAXF 401NL Cytotoxicity assay 4 days Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 25 μM. 22169601
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 25 μM. 30047410
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 24 hrs by spectrophotometry, IC50 = 25 μM. 28487127
HuH7 Antiproliferative assay 48 hrs Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 25 μM. 29057042
A498 Antiproliferative assay 48 hrs Antiproliferative activity against human A498 cells expressing EGFR and Src after 48 hrs by SRB assay, IC50 = 25.6 μM. 26188620
MEXF 1341L Cytotoxicity assay 4 days Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 30.1 μM. 22169601
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay, IC50 = 30.12 μM. 28923383
PXF 1752L Cytotoxicity assay 4 days Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 31.6 μM. 22169601
A549 Cytotoxicity assay 4 to 5 days Cytotoxicity against human A549 cells after 4 to 5 days by MTT assay, IC50 = 33.03 μM. 20466555
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, IC50 = 33.46 μM. 28923383
MDA231 Cytotoxicity assay 4 days Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 34.5 μM. 22169601
LXFL 1121L Cytotoxicity assay 4 days Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 34.6 μM. 22169601
PXF 698L Cytotoxicity assay 4 days Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 36.4 μM. 22169601
PC3 Cytotoxicity assay 4 to 5 days Cytotoxicity against human PC3 cells after 4 to 5 days by MTT assay, IC50 = 36.76 μM. 20466555
HEK293 Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki = 41 μM, IC50 = 44 μM. 22541068
RXF 393NL Cytotoxicity assay 4 days Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 45.6 μM. 22169601
LIXF 575L Cytotoxicity assay 4 days Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 47.2 μM. 22169601
NCI-H23 Cytotoxicity assay 46 hrs Cytotoxicity against human NCI-H23 cells assessed as reduction in cell viability after 46 hrs by MTT assay, IC50 = 49.3 μM. 29138027
polycythemia vera hematopoietic progenitor cell Growth inhibition assay 5 uM Growth inhibition of JAK2 V617F mutant expressing human polycythemia vera hematopoietic progenitor cells at 5 uM by erythroid burst-forming unit assay, NULL = NULL μM. 17178722
A431 Function assay 1 hrs Inhibition of EGF-induced EGFR phosphorylation in human A431 cells pretreated for 1 hrs followed by EGF-stimulation by immunoblot analysis, NULL = NULL μM. 19969465
PC9 Cytotoxicity assay 0.001 to 10 uM 96 hrs Cytotoxicity against human PC9 cells expressing 746-750 sequence deleted EGFR assessed as cell viability at 0.001 to 10 uM after 96 hrs by cell titer-glo assay, NULL = NULL μM. 20222733
NCI-H1975 Cytotoxicity assay 0.001 to 10 uM 96 hrs Cytotoxicity against human NCI-H1975 cells expressing EGFR T790M and L858R mutant at 0.001 to 10 uM after 96 hrs by cell titer-glo assay, NULL = NULL μM. 20222733
Huh7.5 Antiviral assay 30 mins Antiviral activity against Hepatitis C virus J6/JFH infected in human Huh7.5 cells assessed as inhibition of HCV replication pretreated for 30 mins followed by infection measured after 72 hrs by alamar blue dye based fluorescence assay, Activity = NULL μM. 26925208
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells, NULL = NULL μM. 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells, NULL = NULL μM. 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells, NULL = NULL μM. 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells, NULL = NULL μM. 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells, NULL = NULL μM. 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells, NULL = NULL μM. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells, NULL = NULL μM. 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells, NULL = NULL μM. 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells, NULL = NULL μM. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells, NULL = NULL μM. 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells, NULL = NULL μM. 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, NULL = NULL μM. 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells, NULL = NULL μM. 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells, NULL = NULL μM. 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells, NULL = NULL μM. 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, NULL = NULL μM. 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells, NULL = NULL μM. 29435139
HCC827 Apoptosis assay 1 uM 24 hrs Induction of apoptosis in human HCC827 cells at 1 uM after 24 hrs using propidium iodide by flow cytometry, NULL = NULL μM. 24900830
NCI-H1648 Growth inhibition assay IC50 = 0.04002 μM SANGER
TE-12 Growth inhibition assay IC50 = 0.05441 μM SANGER
ECC12 Growth inhibition assay IC50 = 0.08052 μM SANGER
BB30-HNC Growth inhibition assay IC50 = 0.14765 μM SANGER
LB996-RCC Growth inhibition assay IC50 = 0.40161 μM SANGER
EW-24 Growth inhibition assay IC50 = 0.59443 μM SANGER
LC-1F Growth inhibition assay IC50 = 0.60632 μM SANGER
TK10 Growth inhibition assay IC50 = 0.85878 μM SANGER
A388 Growth inhibition assay IC50 = 1.0938 μM SANGER
EKVX Growth inhibition assay IC50 = 1.12354 μM SANGER
TE-9 Growth inhibition assay IC50 = 1.22511 μM SANGER
TE-1 Growth inhibition assay IC50 = 1.4048 μM SANGER
MOLT-16 Growth inhibition assay IC50 = 1.92925 μM SANGER
TE-6 Growth inhibition assay IC50 = 2.5678 μM SANGER
697 Growth inhibition assay IC50 = 2.65305 μM SANGER
A253 Growth inhibition assay IC50 = 2.7516 μM SANGER
OS-RC-2 Growth inhibition assay IC50 = 2.94023 μM SANGER
KS-1 Growth inhibition assay IC50 = 2.94542 μM SANGER
MC116 Growth inhibition assay IC50 = 3.62049 μM SANGER
LB2241-RCC Growth inhibition assay IC50 = 3.81729 μM SANGER
RL95-2 Growth inhibition assay IC50 = 4.0332 μM SANGER
HCE-T Growth inhibition assay IC50 = 4.10188 μM SANGER
NCCIT Growth inhibition assay IC50 = 4.38497 μM SANGER
GCIY Growth inhibition assay IC50 = 4.63532 μM SANGER
LB1047-RCC Growth inhibition assay IC50 = 4.98379 μM SANGER
A3-KAW Growth inhibition assay IC50 = 5.43946 μM SANGER
TE-15 Growth inhibition assay IC50 = 5.4727 μM SANGER
NOS-1 Growth inhibition assay IC50 = 5.49386 μM SANGER
EW-16 Growth inhibition assay IC50 = 6.25387 μM SANGER
LAMA-84 Growth inhibition assay IC50 = 7.00772 μM SANGER
TE-5 Growth inhibition assay IC50 = 7.04247 μM SANGER
HEL Growth inhibition assay IC50 = 7.33564 μM SANGER
NCI-H209 Growth inhibition assay IC50 = 8.04412 μM SANGER
DJM-1 Growth inhibition assay IC50 = 8.52964 μM SANGER
OVCAR-4 Growth inhibition assay IC50 = 8.84219 μM SANGER
NB17 Growth inhibition assay IC50 = 9.25991 μM SANGER
SK-NEP-1 Growth inhibition assay IC50 = 9.35776 μM SANGER
NB5 Growth inhibition assay IC50 = 10.29 μM SANGER
BV-173 Growth inhibition assay IC50 = 10.3272 μM SANGER
MPP-89 Growth inhibition assay IC50 = 10.442 μM SANGER
RPMI-6666 Growth inhibition assay IC50 = 10.4969 μM SANGER
MS-1 Growth inhibition assay IC50 = 11.4658 μM SANGER
ALL-PO Growth inhibition assay IC50 = 11.5179 μM SANGER
NB10 Growth inhibition assay IC50 = 11.7587 μM SANGER
NB13 Growth inhibition assay IC50 = 11.9914 μM SANGER
SCH Growth inhibition assay IC50 = 12.1891 μM SANGER
ES6 Growth inhibition assay IC50 = 12.475 μM SANGER
ETK-1 Growth inhibition assay IC50 = 14.0885 μM SANGER
ES4 Growth inhibition assay IC50 = 14.8445 μM SANGER
K-562 Growth inhibition assay IC50 = 15.814 μM SANGER
D-502MG Growth inhibition assay IC50 = 17.3468 μM SANGER
LB647-SCLC Growth inhibition assay IC50 = 17.7726 μM SANGER
TE-10 Growth inhibition assay IC50 = 18.1138 μM SANGER
MZ1-PC Growth inhibition assay IC50 = 18.3774 μM SANGER
CTB-1 Growth inhibition assay IC50 = 18.5075 μM SANGER
NMC-G1 Growth inhibition assay IC50 = 18.8029 μM SANGER
C2BBe1 Growth inhibition assay IC50 = 18.8664 μM SANGER
SK-PN-DW Growth inhibition assay IC50 = 19.5482 μM SANGER
HCC2157 Growth inhibition assay IC50 = 20.3361 μM SANGER
Becker Growth inhibition assay IC50 = 20.3541 μM SANGER
ST486 Growth inhibition assay IC50 = 20.4093 μM SANGER
LC-2-ad Growth inhibition assay IC50 = 20.9637 μM SANGER
NCI-H747 Growth inhibition assay IC50 = 21.5139 μM SANGER
BE-13 Growth inhibition assay IC50 = 21.8158 μM SANGER
no-11 Growth inhibition assay IC50 = 21.9106 μM SANGER
TE-8 Growth inhibition assay IC50 = 22.6318 μM SANGER
NB6 Growth inhibition assay IC50 = 22.8303 μM SANGER
BB65-RCC Growth inhibition assay IC50 = 22.9623 μM SANGER
SK-UT-1 Growth inhibition assay IC50 = 23.1497 μM SANGER
D-392MG Growth inhibition assay IC50 = 24.2934 μM SANGER
JVM-2 Growth inhibition assay IC50 = 24.5333 μM SANGER
SW954 Growth inhibition assay IC50 = 24.5916 μM SANGER
QIMR-WIL Growth inhibition assay IC50 = 25.1973 μM SANGER
MEG-01 Growth inhibition assay IC50 = 25.9016 μM SANGER
A101D Growth inhibition assay IC50 = 28.7139 μM SANGER
LB831-BLC Growth inhibition assay IC50 = 30.4004 μM SANGER
KGN Growth inhibition assay IC50 = 30.8661 μM SANGER
HC-1 Growth inhibition assay IC50 = 31.3508 μM SANGER
CP66-MEL Growth inhibition assay IC50 = 31.8366 μM SANGER
D-542MG Growth inhibition assay IC50 = 32.4337 μM SANGER
LS-513 Growth inhibition assay IC50 = 33.4844 μM SANGER
DOHH-2 Growth inhibition assay IC50 = 33.6589 μM SANGER
NB69 Growth inhibition assay IC50 = 33.9206 μM SANGER
SW962 Growth inhibition assay IC50 = 35.7217 μM SANGER
J-RT3-T3-5 Growth inhibition assay IC50 = 36.0724 μM SANGER
MONO-MAC-6 Growth inhibition assay IC50 = 36.5359 μM SANGER
MLMA Growth inhibition assay IC50 = 38.652 μM SANGER
HOP-62 Growth inhibition assay IC50 = 39.1765 μM SANGER
LP-1 Growth inhibition assay IC50 = 39.4415 μM SANGER
ONS-76 Growth inhibition assay IC50 = 39.9152 μM SANGER
KNS-42 Growth inhibition assay IC50 = 40.0531 μM SANGER
NCI-H1581 Growth inhibition assay IC50 = 41.1842 μM SANGER
DSH1 Growth inhibition assay IC50 = 42.407 μM SANGER
NCI-H1355 Growth inhibition assay IC50 = 42.839 μM SANGER
D-247MG Growth inhibition assay IC50 = 45.719 μM SANGER
MC-CAR Growth inhibition assay IC50 = 45.9691 μM SANGER
EW-1 Growth inhibition assay IC50 = 47.5624 μM SANGER
GI-ME-N Growth inhibition assay IC50 = 48.1384 μM SANGER
BT-474 Growth inhibition assay IC50 = 48.1738 μM SANGER
LB373-MEL-D Growth inhibition assay IC50 = 48.7563 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Erlotinib HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Targets
HER1/EGFR [1]
(Cell-free assay)
2 nM
In vitro
In vitro Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon cancer cells. [1] Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. [2] Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [3] The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. [4] Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [5]
Kinase Assay Kinase assays
96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colonmetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes.
Cell Research Cell lines A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells
Concentrations 30 nM-20 μM
Incubation Time 72 hours
Method Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Met / Met / p-Axl / Axl / pERK / ERK / pEGFR / EGFR / p-STAT3 / STAT3 / p-Akt / Akt p-Raf-1 / Raf-1 / p-MEK / MEK cleaved PARP / PARP p27 / pS10-p27 / pT157-p27 / pT187-p27 Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Bad / Bim EL / PUMA 28604685
Immunofluorescence Bax / Cyto C E-cadherin / β-catenin / Vimentin EGFR 17927446
Growth inhibition assay Cell viability 30377412
In Vivo
In vivo At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. [1] Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. [5]
Animal Research Animal Models Male 5-week-old BALB-nu/nu with HPAC cells
Dosages 50 mg/kg
Administration Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting
Cirrhosis Liver
University of Texas Southwestern Medical Center|National Cancer Institute (NCI)
 July 2024 Phase 2
NCT06161558 Not yet recruiting
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 1
NCT05827614 Recruiting
Non-small Cell Lung Cancer|Non-Small Cell Lung Adenocarcinoma|Non-Small Cell Squamous Lung Cancer|Head and Neck Squamous Cell Carcinoma|Esophageal Cancer|Gastric Cancer|Breast Cancer|Bladder Cancer|Ovarian Cancer|Endometrial Cancer|Liposarcoma
Boundless Bio
 March 24 2023 Phase 1
NCT03460678 Terminated
Carcinoma Non-Small-Cell Lung
Hikma Pharmaceuticals LLC
 February 28 2018 Phase 4

Chemical Information & Solubility

Molecular Weight 429.90 Formula

C22H23N3O4.HCl
CAS No. 183319-69-9 SDF Download Erlotinib HCl SDF
Smiles COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (13.95 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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Frequently Asked Questions

Question 1:
Whether S1023 is suitable for mouse assays?

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Dissolving S1023 in 15% Captisol is for oral gavage and it's a suspension.

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