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].

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 *A+, Brian T. Campbell A+, Mark W. Holladay A+, Julia M. Ford Pulido A?, Helen Hua A?, Dana Gitnick , Michael F. Gardner , Joyce James , Mike A. Breider , Daniel Brigham A?, Barbara Belli A?, Robert C. Armstrong A?, 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 997A–1002