A PDGFR family kinase inhibitor
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)
Animal experiment: | Mice: The antitumor efficacy of AC710 is assessed in a subcutaneous flank-tumor xenograft model in athymic nude mice using the MV4-11cell line. AC710 is dosed at 0.3, 3, and 30 mg/kg for 2 weeks. Tumor growth and body weight is monitored[1]. |
参考文献: [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002. | |
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