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

Inhibitors

Cat.No.  Name Information
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.
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).
M1749 Gefitinib Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages.
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.
M1913 Neratinib Neratinib (HKI-272) is an orally available, irreversible inhibitor of Her 2 tyrosine kinase.
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 a fourth generation allosteric inhibitor of mutant EGFR, which inhibits EGFR at 10 μM ATP, EGFRL858R, EGFRT790M and EGFRL858R/T790M with IC50 values of 1.9, 0.019, 0.19 and 0.002 μM respectively.
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 Zoligratinib 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 novel antihistamine compound whose peripheral Hi-antagonist has the same potency as trichloropyridine, but doses of up to 4mg of atorvastatin do not reduce alert performance or increase response time. 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 Osimertinib mesylate (AZD-9291 mesylate) Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
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.



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