AC-710 is an inhibitor of PDGFR family kinases (IC50s = 7.7, 10.5, 2, and 1.2 nM for PDGFRβ, CSF1R, FLT3, and c-Kit, respectively).1 It is greater than 30-fold selective for PDGFR family kinases over a panel of 386 kinases, as well as over a panel of five cytochrome P450 (CYP) enzymes (IC50s = >40 ?M). AC-710 (30 mg/kg) inhibits CSF1R-dependent M-NFS-60 murine leukemia cell proliferation and reduces tumor volume in an FLT3 mutant MV4-11 leukemia mouse xenograft model.
1.Liu, G., Campbell, B.T., Holladay, M.W., et al.Discovery of AC710, a globally selective inhibitor of platelet-derived growth factor receptor-family kinasesACS Med. Chem. Lett.3(12)997-1002(2012)