Erlotinib mesylate (CP-358774, OSI-774, NSC 718781) is a potent, selective inhibitor of EGFR with IC50 of 2 nM.
Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM.
Erlotinib inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentrations in cell culture and blocks cell cycle progression at the G1 phase.
Erlotinib 100mg/kg completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice; orally active.
