Pelitinib

A potent, selective, orally active, irreversible inhibitor of EGFR with IC50 of 80 nM; inhibits autophosphorylation of the cytoplasmic domain of HER-2 with IC50 of 1.23 uM; shows 1-3 orders of magnitude higher IC50 value for Src, Cdk4, c-Met, Raf, and MEK/ERK; inhibits proliferation in NHEK, A431, and MDA-468 cells (IC50= 61, 125, and 260 nM, respectively) ; potently inhibits the EGFR phosphorylation in A431 xenografts, suppresses tumorigenesis in APCMin/+ mice.Lung Cancer Phase 2 Clinical.