CL-387785

Research use only, not for human use.

CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50： 370+/-120 pM);is able to overcome resistance caused by the T790M mutation on a functional level.

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 = 31-125 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.

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CL387785 | CL 387785 | CL-387785

Angiogenesis

VEGFR

EGFR

Cancer

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194423-06-8

381.23

C18H13BrN4O

>98% (HPLC)

DMSO : 13.67 mg/mL 35.86 mM;

CC#CC(=O)Nc1cc2c(cc1)ncnc2Nc1cc(ccc1)Br

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

(-20℃)

With Ice Pack

≥ 2 years