S81294 |
GSK343 |
源叶(MedMol) | 99% |
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- 产品描述: GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
- 靶点: IC50: 4 nM (EZH2), 240 nM (EZH1);HistoneMethyltransferase; Autophagy
- 体内研究:
Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels
- 参考文献:
1. Sharad K, et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. 2. Ding M, et al. The polycomb group protein enhancer of zeste 2 is a novel therapeutic target for cervical cancer. Clin Exp Pharmacol Physiol. 2015 May;42(5):458-64.
- 溶解性: DMSO : 15.62 mg/mL (28.84 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.846 ml 9.23 ml 18.461 ml 5 mM 0.369 ml 1.846 ml 3.692 ml 10 mM 0.185 ml 0.923 ml 1.846 ml 50 mM 0.037 ml 0.185 ml 0.369 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)