TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
CAS：1361951-15-6
分子式：C22H25F3N4O
分子量：418.46
纯度：98%
存储：Store at -20°C

Background:

TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.

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[1].

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[1].

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.