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CL-387785 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. Uses: Protein kinase inhibitors. Synonyms: CL-387785; CL 387785; CL-387,785; CL387785; EKI-785; EKI 785; EKI785. Grades: 0.98. CAS No. 194423-06-8. Molecular formula: C18H13BrN4O. Mole weight: 381.233. BOC Sciences 8
WZ-8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. WZ8040 is about 30-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than other quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ-8040 may be clinically more effective and better tolerated than quinazoline-based inhibitors. Synonyms: WZ8040; WZ 8040. Grades: 0.98. CAS No. 1214265-57-2. Molecular formula: C24H25ClN6OS. Mole weight: 481.015. BOC Sciences 10

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