| 产品描述： | SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells |
| 靶点： |
IC50: 8 nM (RET) |
| 体外研究： |
SPP86 (0-10 μM) inhibits MAPK signaling and proliferation in RET/PTC1 expressing TPC1 but not 8505C or C643 cells. SPP86 (0-10 μM) inhibits RET- induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling and estrogen receptorα (ERα) phosphorylation in MCF7 cells. Western Blot Analysis Cell Line: Thyroid cancer derived cell lines expressing the RET/PTC1 rearrangement (TPC1), BRAFV600E (8505C) or RASG13R (C643) mutations. Concentration: 0-10 μM. Incubation Time: 90 min. Result: Inhibited RET- induced ERK1/2 phosphorylation in thyroid cancer cell lines. Western Blot Analysis Cell Line: MCF7 cells (human breast cancer). Concentration: 0-10 μM. Incubation Time: 30 min. Result: Inhibited RET- induced ERα phosphorylation and proliferation in MCF7 cells. |
| 参考文献： |
1. Alao JP, Michlikova S, Dinér P, Grøtli M, Sunnerhagen P. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer. 2014 Nov 20;14:853. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.606 ml |
18.029 ml |
36.058 ml |
| 5 mM |
0.721 ml |
3.606 ml |
7.212 ml |
| 10 mM |
0.361 ml |
1.803 ml |
3.606 ml |
| 50 mM |
0.072 ml |
0.361 ml |
0.721 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)
