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

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

EKI-785； WAY-EKI 785

Off-white to yellow solid

DMSO : 13.67 mg/mL (35.86 mM)

EGFR

CL-387785 blocks EGF-stimulated autoposphorylation of the receptor in cells (IC50, 5 nM), In cell lines that overexpress EGF-R or c-erbB-2, CL-387785 inhibits cell proliferation (IC50, 31 nM) primarily in a cytostatic manner.

In nude mice overexpressed EGF-R, CL-387785 (80 mg/kg/day, p.o.) profoundly blocks the growth of tumor. In murine models of autosomal recessive polycystic kidney disease (ARPKD), treatment of Balb/c-bpk/bpk (BPK) mice with CL-387785 (90 mg/kg, i.p.) results in a marked reduction of collecting tubule cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and prolonged life span. Doses of CL-387785 as low as 25 mg/kg reduces the growth of HCA-7-induced xenograft tumor, and a dose of 100 mg/kg prevents tumor growth entirely. Dose of 50 mg/kg CL-387785 is effective at reducing the growth of HCT-116-induced xenograft tumor.