S89397 |
SPP-86 |
源叶(MedMol) | 98% |
- 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: -20℃
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)