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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.
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 is a chimeric IgG1 monoclonal antibody to EGFR that inhibits the interaction of EGFR with its ligand. For use in cellular assays, human IgG antibody can be used as an isotype control. (For human and non-humanized mice).
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.



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