AC710 is a potent PDGFR inhibitor with Kds of 0.6 nM for FLT3, 1 nM for KIT, 1.57 nM for CSF1R, 1.3 nM for PDGFRα, and 1 nM for PDGFRβ.

PDGFRα:1.3 nM (Kd), FLT3:0.6 nM (Kd), c-Kit:1 nM (Kd), CSF1R:1.57 nM (Kd), PDGFRβ:1 nM (Kd)

At a dosage of 0.3 mg/kg, AC710 transiently inhibits tumor growth, with rapid resumption following cessation. Doses of 3 and 30 mg/kg result in complete tumor regression and prolonged suppression of tumor volume post-treatment. Notably, administration of AC710 does not lead to bodyweight loss in treated animals across all tested doses. Further, AC710 significantly mitigates disease progression in a mouse collagen-induced arthritis (CIA) model in a dose-dependent manner, starting from a low dose of 3 mg/kg over a span of 15 days (day 0-14). At increased dosages of 10 and 30 mg/kg, AC710's effectiveness in reducing joint swelling and inflammation is comparable or slightly superior to that of dexomethasone administered at a safe dose.

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 are monitored.