Chemical Name: (2E)-N-[4-[[3-Chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide. Alternate Names: HKI-272
Dual EGFR and HER2 inhibitor
Molecular Weight:
557.05
Purity:
>98% by HPLC NMR (Conforms)
Form:
White solid
CAS Number:
[698387-09-6]
Formula:
C30H29ClN6O3
Application Notes:
Neratinib is a potent, irreversible inhibitor of HER2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50s= 59 nM and 92 nM, respectively). It suppresses receptor autophosphorylation and proliferation, blocks cell-cycle progression and inhibits HER2 signaling in of EGFR-dependent cancer cells and tumor xenograft models.1 Neratinib inhibits proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR.2 Synergizes with dasatinib in HER2-positive cancer cells and xenografts.3 Its been shown to also inhibit MST1 (IC50 = 37.7 nM).4
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