S82943 |
AC710 |
| 源叶(MedMol) | 95% |
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- 产品描述： AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
- 靶点： PDGFRα:1.3 nM (Kd);PDGFRβ:1 nM (Kd);c-Kit:1 nM (Kd);FLT3:0.6 nM (Kd);CSF1R:1.57 nM (Kd)
- 体内研究： 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 body weight loss is observed in animals treated with AC710 at all doses, indicating that it is well tolerated in mice at efficacious 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. AC710 is well tolerated at the tested doses
- 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.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.777 ml 8.886 ml 17.771 ml 5 mM 0.355 ml 1.777 ml 3.554 ml 10 mM 0.178 ml 0.889 ml 1.777 ml 50 mM 0.036 ml 0.178 ml 0.355 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
