Description
A potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5nM and 9.0nM in autophosphorylation assay; displays no activity to PDGFR, FGFR, InsR, PKC, and CDK1/2/4; suppresses heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3 and erbB4 with IC50 of 5, 14 and 10nM, respectively, also inhibits expression of pp62c-fos in response to heregulin; shows high in vivo activity against A431 xenografts. Lung Cancer Discontinued