| 产品描述： | BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively). |
| 靶点： |
JAK2:1.1 nM (IC50);Tyk2:66 nM (IC50);JAK1:75 nM (IC50);JAK3:360 nM (IC50);TyrosineKinases;HistoneMethyltransferase;JAK |
| 体内研究： |
BMS-911543 is well tolerated up to 100 mg/kg in rats (mean AUC0-72 h, 11300 μM·h) and dogs (AUC0-24 h, 610 μM·h). A 15 mg/kg/day dose (Day 14 AUC0-24 h, 3200 μM·h) is well tolerated in two-week repeat dose studies in rats. BMS-911543 (30 mg/kg, p.o.) suppresses the growth of tumor and prolongs the median survival in KPC-Brca1 mice. BMS-911543 also selectively reduces pSTAT5 expression in pancreatic tumors and decreases levels of intratumoral FoxP3+ T regulatory cells in mice administered BMS-911543 |
| 参考文献： |
1. Wan H, et al. Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. 2. Mace TA, et al. Single agent BMS-911543 Jak2 inhibitor has distinct inhibitory effects on STAT5 signaling in genetically engineered mice with pancreatic cancer. Oncotarget. 2015 Dec 29;6(42):44509-22. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.312 ml |
11.56 ml |
23.12 ml |
| 5 mM |
0.462 ml |
2.312 ml |
4.624 ml |
| 10 mM |
0.231 ml |
1.156 ml |
2.312 ml |
| 50 mM |
0.046 ml |
0.231 ml |
0.462 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