AC710 is a potent, orally active, and selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity. Its 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.. AC710 causes tumor regression of leukemia cell xenografts in mice. AC710 also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. AC710 is now a preclinical development candidate.
REFERENCES:
Liu *†, Brian T. Campbell †, Mark W. Holladay †, Julia M. Ford Pulido ‡, Helen Hua ‡, Dana Gitnick , Michael F. Gardner , Joyce James , Mike A. Breider , Daniel Brigham ‡, Barbara Belli ‡, Robert C. Armstrong ‡, and Daniel K. Treiber. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med. Chem. Lett., 2012, 3 (12), pp 997–1002