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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