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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
M9737 Pyrotinib Pyrotinib (SHR-1258) is an orally bioavailable, potent and selective EGFR/HER2 dual inhibitor, with IC50 values of 13 and 38 nM, respectively.
M9722 Tyrphostin AG528 Tyrphostin AG528 (Tyrphostin B66) is an inhibitor of EGFR and ErbB2 with IC50 values of 4.9 and 2.1 μM, respectively.
M9711 AG1557 AG1557 is a potent and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with pIC50 value of 8.194.
M9709 NSC228155 NSC228155 is an activator of EGFR, which binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR.
M9686 Tarloxotinib bromide Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
M9642 EGFR inhibitor 324674 EGFR inhibitor 324674 is a cell permeable, potent and selective EGFR inhibitor with IC50 of 21 nM.
M9535 Mobocertinib Mobocertinib (TAK-788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions.
M9534 TAS6417 TAS6417 is a novel EGFR inhibitor targeting exon 20 insertion mutations, with IC50 values range from 1.1-8.0 nM.
M9400 AST2818 mesylate AST2818 mesylate is a third generation EGFR inhibitor that targets both EGFR activating mutations and T790M thus leading to tumor growth inhibition.
M9132 ABM-3627 ABM-3627, also known as Mutant EGFR inhibitor, is a selective and potent Mutated EGFR inhibitor.
M8818 Tyrphostin RG 13022 RG13022 is a non-phenolic tyrphostin-class tyrosine kinase inhibitor.
M6411 AG 494 AG 494 is a potent EGFR-kinase inhibitor with an IC50 value of 1 µM in HT-22 cells.
M6221 Pertuzumab Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.
M6218 Trastuzumab Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD.
M6103 Cetuximab Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation.
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.
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).
M4585 Taxifolin Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.
M4208 (-)-Epigallocatechin gallate (-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoid form green tea, and inhibits the activation of EGFR, HER2 and HER3, with antitumor activity.
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 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.


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