TP-3654 |
| Catalog No.GC19361 |
TP-3654는 Pim-1 및 Pim-3에 대해 각각 Ki 값이 5 및 42nM인 2세대 Pim 키나제 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1361951-15-6
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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