GSK2126458-其他小分子化合物-深圳欣博盛生物科技有限公司

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GSK2126458

品牌：Adipogen

官网链接

说明书

折扣/货期

货号：SYN-1126-M001	规格：1 mg	目录价：￥2198
货号：SYN-1126-M005	规格：5 mg	目录价：￥3332
货号：SYN-1126-M010	规格：10 mg	目录价：￥5292
货号：SYN-1126-M050	规格：50 mg	目录价：￥15876
货号：SYN-1126-M100	规格：100 mg	目录价：￥询价

产品详情

* 以下信息仅供参考，详情请以原厂网站为准

产品名称:

GSK2126458

别名:

HYR-582

产品描述:

GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-alpha (p85alpha/p110alpha) with IC(50) of 0.04nM. GSK2126458 has Ki values in the picomolar range for each of the class I PI3K isoforms and MTOR1/2 complexes. GSK2126458 has potent in vitro and in vivo growth-inhibitory effects on cancer cells. In comparison with other clinical PI3K inhibitors, GSK2126458 is around 100-fold more potent than BEZ235 (6nM). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110R ( E542K, E545K, and H1047R ) with Ki of 0.008nM, 0.008nM and 0.009nM in human cancer. In mechanistic cellular assays, GSK2126458 caused a significant reduction in the levels of pAKT-S473 with remarkable potency. Consistent with its activity against both PI3K R and mTOR, GSK2126458 also inhibits phosphorylation of AKT-T308 and p70S6K at low nanomolar concentrations. GSK2126458 induces a G1 cell cycle arrest and inhibits cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines.

保存温度:

+4°C

运输温度:

Ambient

预期分子量:

505.5

产品形式:

solid

产地:

瑞士

纯度:

>95%