| 产品描述： | CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity |
| 靶点： |
IC50: < 25 nM (NAMPT);Apoptosis;NAMPT |
| 体内研究： |
A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of CHS-828 (GMX1778) at a dose of 150 mg/kg or 650 mg/kg in the NAPRT1-deficient xenograft experiments. CHS-828 (GMX1778) at 650 mg/kg is above the maximum tolerated dose. The administration of NA as a 4-h iv infusion immediately following treatment with 750 mg/kg CHS-828 (GMX1778) reduced the mortality associated with toxic doses of GMX1777 |
| 参考文献： |
1. Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29(21):5872-88. 2. Cerna D, et al. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner |
| 溶解性： |
DMSO : ≥ 39 mg/mL (104.88 mM) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.689 ml |
13.446 ml |
26.891 ml |
| 5 mM |
0.538 ml |
2.689 ml |
5.378 ml |
| 10 mM |
0.269 ml |
1.345 ml |
2.689 ml |
| 50 mM |
0.054 ml |
0.269 ml |
0.538 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京