S82991 |
TP-3654 |
源叶(MedMol) | 99% |
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- 产品描述: TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
- 靶点: Ki: 5 nm(Pim-1), 239 nM (Pim-2), 42 nM (Pim-3);Pim
- 体外研究:
TP-3654 demonstrates potent PIM-1 specific cellular activity in the PIM-1/BAD overexpression system with an average EC50 of 67 nM. TP-3654 treatment reduces levels of phospho-BAD in vitro using the bladder cancer cell line UM-UC-3. TP-3654 reduces colony growth of T24 and UM-UC3 cells, confirming the PIM-1–dependent growth for both cell lines
- 体内研究:
Oral dosing of 200 mg/kg TP-3654 significantly reduces both UM-UC-3 and PC-3 tumor growth measured by volume (caliper) and by final tumor weight, with no significant changes in body weight or gross adverse toxicity
- 参考文献:
1. Foulks JM, et al. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Neoplasia. 2014 May;16(5):403-12.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.39 ml 11.949 ml 23.897 ml 5 mM 0.478 ml 2.39 ml 4.779 ml 10 mM 0.239 ml 1.195 ml 2.39 ml 50 mM 0.048 ml 0.239 ml 0.478 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)