Catalog

EGFR/HER2 Epidermal growth factor receptor/Human epidermal growth factor receptor-2

Inhibitors

Cat.No.	Name	Information
M6081	EAI045	EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
M5679	Gefitinib HCl	Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.
M5621	Erlotinib	Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
M5346	WZ3146	WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
M5318	CH5183284	CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
M5307	Afatinib dimaleate	Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.
M5286	Acrivastine	Acrivastine is a new antihistamine with peripheral HI-antagonist potency equal to that of triprolidine, but in doses up to 4 mg acrivastine does not impair performance on a vigilance task or increase. reaction time.
M5275	Nazartinib	Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.
M5169	EAI045	EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
M5164	AZD3759	AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively.
M5133	Olmutinib	Olmutinib is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK).
M5127	FIIN-2	FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.
M5099	AZD-9291 (Mesylate)	AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).
M5031	Poziotinib	Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.
M4871	CL-387785	CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.
M4850	PD153035	PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
M4805	BIBX 1382	BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
M4002	Chrysophanic acid	Chrysophanic acid, also known as chrysophanol, is a fungal isolate and a natural anthraquinone with anti-cancer activity.
M3780	XL647	XL647 is an extremely potent and selective inhibitor of EGFR phosphorylation (IC50 = 0.3 nM).
M3689	PD153035 hydrochloride	PD153035 hydrochloride is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
M3684	Canertinib dihydrochloride	Canertinib 2HCl is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4.
M3569	AST-1306	AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases,
M3560	ARRY-380	ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.
M3553	TAK-285	TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
M3517	Lapatinib	Lapatinib, used in the form of Lapatinib ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
M3491	OSI-420	OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
M3238	4-Quinazolinamine	4-Quinazolinamine (4-Aminoquinazoline) is a potent and highly selective EGFR tyrosine kinase inhibitor.
M3217	AV-412	AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor.
M3199	Varlitinib	ARRY334543 is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively.
M3098	Tyrphostin AG 879	Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
M2916	PD168393	PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
M2464	BMS-690514	BMS-690514 is a potent inhibitor of EGFR and VEGFR2 with IC50 of 5 nM and 50 nM, respectively.
M2424	AZD9291	AZD9291 is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively.
M2312	AG-1478	AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM.
M2255	Genistein	Genistein is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.
M2212	CO-1686	CO-1686 is a potent, novel inhibitor of EGFR L858R/T790M kinase with Ki of 21.5 nM and 303.3 nM, respectively.
M2117	CNX-2006	CNX-2006 is a novel irreversible EGFR inhibitor with IC50 value of <20 nM.
M2021	AG 18	AG-18 is an inhibitor of EGF receptor kinase with an IC50 value of 35 μM.
M1943	Canertinib	Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).
M1919	Mubritinib	Mubritinib (TAK-165) is a new potent inhibitor of human epidermal growth factor receptor 2 (HER2) tyrosine kinase (IC50 = 6 nM).
M1913	Neratinib	Neratinib (HKI-272) is an orally available, irreversible inhibitor of Her 2 tyrosine kinase.
M1904	Pelitinib	Pelitinib (EKB-569) is an irreversible EGFR tyrosine kinase inhibitor with IC50 of 38.5 nM.
M1875	PD173074	PD173074 is a selective FGFR1 and FGFR3 inhibitor with IC50 values of 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively.
M1869	Dacomitinib	Dacomitinib (PF-00299804) is an oral, irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases.
M1851	WZ8040	WZ8040 is a novel EGFR inhibitor which suppresses the growth of EGFR-T790M-containing cell lines and inhibits EGFR phosphorylation.
M1850	WZ4002	WZ4002 is a novel, selective EGFR kinase inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) with IC50 of 8 nM.
M1802	Lapatinib Ditosylate	Lapatinib Ditosylate (CAS 388082-78-8) is a selective and effective inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM) and ErbB-4 kinase (Ki = 347 nM).
M1784	Icotinib	Icotinib (BPI-2009H) is a potent and novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC50 of 5 nM.
M1749	Gefitinib	Gefitinib (ZD-1839, Iressa) is a novel potent EGFR tyrosine kinase inhibitor with an IC50 of 0.40nM.
M1721	AZD4547	AZD4547 is a potent, selective and orally active pan-FGFR inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.

EGFR/HER2 Epidermal growth factor receptor/Human epidermal growth factor receptor-2

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