Epertinib is an inhibitor of EGFR, HER2, and HER4 (IC50s = 1.48, 7.15, and 2.49 nM, respectively). It is selective for these kinases over VEGFR2, insulin-like growth factor 1 receptor (IGF-1R), c-Src, KIT, and PDGFRbeta (IC50s = >10,000 nM for all). Epertinib inhibits EGFR and HER2 autophosphorylation in NCI N87...

Description: Epertinib hydrochloride (S-22611 hydrochloride) shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Target: EGFR, HER. Smiles:...