| 产品描述： | SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells |
| 靶点： |
DOT1L:0.3 nM (IC50);HistoneMethyltransferase |
| 体内研究： |
SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors |
| 参考文献： |
1. Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. 2. Zhang X, et al. Prognostic and therapeutic value of disruptor of telomeric silencing-1-like (DOT1L) expression in patients with ovarian cancer. J Hematol Oncol. 2017 Jan 23;10(1):29. 3. Zhang L, et al. Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Oncotarget. 2014 Nov 15;5(21):10665-77. |
| 溶解性： |
DMSO : 50 mg/mL (80.83 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.617 ml |
8.083 ml |
16.166 ml |
| 5 mM |
0.323 ml |
1.617 ml |
3.233 ml |
| 10 mM |
0.162 ml |
0.808 ml |
1.617 ml |
| 50 mM |
0.032 ml |
0.162 ml |
0.323 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