Crenolanib (CP-868596)(AB273385)

MW 443.5 Da, Purity =97%. Potent inhibitor of PDGFR (Kd for alpha = 2.1 nM; beta = 3.2 nM) and FLT3 (Kd = 0.74 nM). Type I inhibitor that binds only the active kinase conformation. Active towards imatinib-resistance assciated PDGFR-alpha mutations (D842I, D842V, D842Y, DI842-843M, and deletion I843). Active against FLT3/ITD and FLY3/D835 mutatants. Over 100-fold selective for PDGFR versus c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.