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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
有效期:
Stable for at least 2 years after receipt when stored at -20°C.
产地:
瑞士
纯度:
>95%
CAS号:
1086062-66-9
分子式:
C25H17F2N5O3S
溶解度:
Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
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