crenolanib-besylate

Description: Crenolanib (formerly also known as CP-868596) is a novel, potent, orally bioavailable and selective small molecule inhibitor of platelet-derived growth factor receptor PDGFRalpha/beta with Kd of 2.1 nM/3.2 nM in CHO cells, it also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, > 100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib has potential anticancer activity by binding to and inhibiting PDGFR, which may result in the inhibition of PDGFR-related signal transduction pathways, and, so, the inhibition of tumor angiogenesis and tumor cell proliferation.

References: Clin Cancer Res. 2012 Aug 15; 18(16):4375-84

Related CAS: 670220-93-6 (Crenolanib besylate)