CL-387785

Overview

CL-387785, also known as EKI-785, is an 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 = 31-125 nM) 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). CL-387,785 is useful for studying the interaction of small molecules with EGF-R and may have clinical utility.

Application

Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cardiovascular and blood system | EGFR

Product Information

• Catalog No.: B0084-458793
• CAS No.: 194423-06-8
• Molecular Formula: C18H13BrN4O
• Molecular Weight: 381.233
• Purity: 0.98

Source

Original product source