cl-387785-eki-785

Description: CL-387785 (CL387785; WAY-EKI 785; EKI 785; EKI785) is a novel, potent, covalent / irreversible, and selective EGFR inhibitor with potential anticancer activity. It inhibits EGFR with an IC50 of 370 pM. CL-387785 acts by covalently binding to EGFR and blocking EGF-stimulated autophosphorylation of the receptor in cells (IC50 approximately 5 nM), thus inhibiting 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.

References: Biochem Pharmacol. 1999 Apr 15; 57(8):917-25; Proc Natl Acad Sci U S A. 2002 Feb 5; 99(3):1521-6.

Chemical Name: N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide

SMILES Code: CC#CC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O