CL-387785

CAS No.	194423-06-8	Cat. No.	BCP10214
Name	CL-387785
Synonyms	CL 387785;CL387785;EKI-785;EKI 785;EKI785;WAY-EKI 785;WAY EKI 785;WAYEKI 785;
Formula	C18H13BrN4O	M. Wt	381.23

Description	in vitro: CL-387785 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 . Whereas transformation by most EGFR mutants confers on cells sensitivity to erlotinib and gefitinib, transformation by an exon 20 insertion makes cells resistant to these inhibitors but more sensitive to the irreversible inhibitor CL-387,785. CL-387,785 is able to overcome resistance caused by the T790M mutation on a functional level, correlating with effective inhibition of downstream signaling pathways. in vivo: CL-387785 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). Treatment of BPK mice with EKI-785 resulted in a marked reduction of collecting tubule (CT) cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and an increa
Pathways	Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway
Targets	EGFR

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