Neratinib (HKI-272) is a potent, highly selective, irreversible HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays.
Neratinib (HKI-272) weakly inhibits KDR and Src (IC50=0.8 and 1.4 uM), no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met.
Neratinib (HKI-272) inhibits downstream signal transduction events and cell cycle regulatory pathways, leads to arrest at the G(1)-S phase transition, decreases cell proliferation.
Neratinib (HKI-272) is active in HER-2- and EGFR-dependent tumor xenograft models, orally bioavailable.
