| 产品描述： | Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM. |
| 靶点： |
Ki: < 80 pM (DOT1L histone methyltransferase);HistoneMethyltransferase |
| 体内研究： |
Pinometostat (EPZ-5676) (70 mg/kg, i.p.) causes complete and sustained regression in a rat xenograft model of MLL-rearranged leukemia. Pinometostat (EPZ-5676) (70, 35 mg/kg, i.v.) reduces HOXA9 and MEIS1 mRNA levels of tumors taken from rats, and reduces MLL-fusion target gene expression in vivo |
| 参考文献： |
1. Daigle SR, et al. Potent inhibition of DOT1L as treatment for MLL-fusion leukemia. Blood. 2013 Jun 25. [Epub ahead of print 2. Klaus CR, et al. DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells. J Pharmacol Exp Ther. 2014 Sep;350(3):646-56. |
| 溶解性： |
DMSO : 100 mg/mL (177.71 mM; Need ultrasonic) Ethanol : 100 mg/mL (177.71 mM; Need ultrasonic) |
| 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 |
|
| 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