AC 710, Potent and selective PDGFR family inhibitor, Each

Details

AC 710 is a potent PDGFR family inhibitor (IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively; Kd = 1.3 nM for PDGFRα). Exhibits >30-fold selectivity over a panel of other kinases and exhibits no activity against cytochrome P450. Causes tumor regression of leukemia cell xenografts in mice. Also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. Orally active.