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TP-3654
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TP-3654图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TP-3654 是第二代 Pim 激酶抑制剂,对 Pim-1 和 Pim-3 的 Ki 值分别为 5 和 42 nM。

Cell experiment:

50% from the initial screen are performed using 10-dose, three-fold serial dilutions of TP-3654 starting with 10 μM at Km ATP concentrations for each kinase[1].-->1 μM TP-3654 is tested against 336 kinases at a concentration of 10 μM ATP. IC50 determinations of phosphoinositide 3-kinase (PI3K) (α, β, δ, and γ) and all kinases inhibited by >50% from the initial screen are performed using 10-dose, three-fold serial dilutions of TP-3654 starting with 10 μM at Km ATP concentrations for each kinase[1].

Animal experiment:

When tumors of mice reaches 100 to 200 mm3 by caliper measurement, mice are randomized, and oral dosing of TP-3654 or vehicle control began and continued every day for 5 days with 2 days off for 18 to 21 days. Tumor volumes and body weights were determined twice a week[1].

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.

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.