| 产品描述： | BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively |
| 靶点： |
TGF-β Receptor;TGF-beta/Smad |
| 体外研究： |
BMS-986260 is a highly potent TGFβR1 inhibitor in both human (Kiapp=0.8 nM) and mouse (Kiapp= 1.4 nM) biochemical assays. BMS-986260 also inhibits TGFβ induced SMAD phosphorylation in NIH3T3 cell line, primary human T cells, and mouse and human whole blood. BMS-986260 inhibits TGF-β mediated induction of regulatory T cell (Treg) by downregulation of FOXP3 expression and a repression of CD25 with an IC50 of 230 nM |
| 参考文献： |
1. Velaparthi U, et al. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett. 2020;11(2):172-178. Published 2020 Jan 28. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.612 ml |
13.062 ml |
26.124 ml |
| 5 mM |
0.522 ml |
2.612 ml |
5.225 ml |
| 10 mM |
0.261 ml |
1.306 ml |
2.612 ml |
| 50 mM |
0.052 ml |
0.261 ml |
0.522 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