AC710是一种 PDGFR 抑制剂,能够作用于 FLT3 (Kd:0.6),CSF1R (Kd:1.57),KIT (Kd:1),PDGFRα (Kd:1.3) 和 PDGFRβ (Kd:1.0)。
产品描述
AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
体内活性
At 0.3 mg/kg of AC710, tumor growth is temporally inhibited, and growth resumes quickly thereafter. At 3 and 30 mg/kg of AC710, tumors regress completely, and the tumor volume stays suppressed for an extended period after dosing is halted. No bodyweight loss is observed in animals treated with AC710 at all doses. AC710 exhibits a significant impact on disease in a dose-dependent fashion in a mouse collagen-induced arthritis (CIA) model, at a dose as low as 3 mg/ kg for 15 days (day 0-14). At 10 and 30 mg/kg, AC710 demonstrates equivalent or slightly better efficacy in reducing the joint swelling and inflammation than dexomethasone administered at a safe dose.
动物实验
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.
Cas No.
1351522-04-7
分子式
C31H42N6O4
分子量
562.7
储存和溶解度
DMSO:15 mg/mL (26.66 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years