CL-387785 (EKI-785) CAS :194423-06-8

CL-387785,also known as EKI-785,is a n irreversible inhibitor of EGF-receptor (EGFR)kinase activity in vivo(IC50=250-490 pM).CL-387785 covalently bound to EGF-R.It also specifically inhibited kinase activity of the protein(IC50 =370+/-120 pM),blocked EGF-stimulated autophosphorylation of the receptor in cells(ic50 approximately 5 nM),inhibited cell proliferation(IC50=31-125nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2,and profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice(when given orally at 80 mg/kg/day for 10 days,daily).

msds---CL-387785 (EKI-785)