Canertinib dihydrochloride (CI-1033, PD183805) is a potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay.
Canertinib dihydrochloride (CI-1033, PD183805) is a potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay.
Canertinib dihydrochloride (CI-1033, PD183805) displays no activity to PDGFR, FGFR, InsR, PKC, and CDK1/2/4.
Canertinib dihydrochloride (CI-1033, PD183805) suppresses heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3 and erbB4 with IC50 of 5, 14 and 10 nM, respectively, also inhibits expression of pp62c-fos in response to heregulin.
Canertinib dihydrochloride (CI-1033, PD183805) shows high in vivo activity against A431 xenografts.
