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Abmole Inhibitor Catalog 2017

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

Inhibitors

Cat.No.  Name Information
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.
M1705 Erlotinib Hydrochloride Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM).
M1699 CP-724714 CP-724714 is a potent and selective orally active HER-2 tyrosine kinase inhibitor, IC50 = 3 nM.
M1684 BMS-599626 BMS-599626 (AC480) is an orally bioavailable pan-HER tyrosine kinase inhibitor with potential antineoplastic activity.

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