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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.
M11448 BLU-945 Blu-945 is a potent inhibitor of selective epidermal growth factor receptor (EGFR).
M11447 Sunvozertinib Sunvozertinib (DZD9008) is an effective inhibitor of ErbBs (EGFR, Her2, especially mutants) and BTK.
M11417 (S)-Sunvozertinib (S)-Sunvozertinib ((S)-DZD9008) is the S-enantiomer of Sunvozertinib, EGFR exon 20 NPH and ASV insertion, EGFR L858R/T790M mutation and Her2 exon 20 YVMA insertion (IC50 was 51.2 nM, 51.9 nM, 1 nM and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
M11415 (Rac)-JBJ-04-125-02 (Rac)-JBJ-04-125-02 is a racemate of JBJ-04-125-02, which is a potent, selectively mutated, allosteric and oral active EGFR inhibitor. The IC50 of EGFRL858R/T790M was 0.26 nM.
M10787 AZ7550 Mesylate AZ7550 Mesylate is an active metabolite of AZD9291, AZ7550 inhibits IGF1R activity,IC50 1.6 μM.
M10709 TAS0728 TAS0728 is an effective, selective, oral, irreversible, covalently bound HER2 inhibitor covalently bound to the C805 site of HER2, inhibiting its activity.IC50 The value is 13 nM. TAS0728 to BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and HUMAN HER2 IC50 The values are 4.9, 8.5, 31, 65, 33, 25, 86, and 36 nM, respectively. TAS0728 simultaneously inhibits phosphorylation of HER2, HER3 and its downstream effector proteins. Has antitumor activity.
M10509 TX1-85-1 TX1-85-1 is an ErbB3 inhibitor with IC50 of 23 nM, it is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3.
M10472 AZD3759 hydrochloride AZD3759 hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
M10337 Avitinib (AC0010) Avitinib (Abivertinib; AC0010) is a third-generation irreversible EGFR tyrosine kinase inhibitor, with potential antineoplastic activity.
M10038 Irbinitinib (Tucatinib) Tucatinib, also known as Irbinitinib and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (HER2).
M9938 Lazertinib Lazertinib, also known as YH-25448 and GNS-1480, is an oral active, highly potent, mutant-selective and irreversible EGFR Tyrosine-kinase inhibitors (TKIs) targets both the T790M mutation and activating EGFR mutations while sparing wild type-EGFR.
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.



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