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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-Akt-Uprosertib
Uprosertib

Chemical Structure : Uprosertib

CAS No.: 1047634-65-0

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Uprosertib (GSK2141795, GSK-2141795)

货号: PC-27801Not For Human Use, Lab Use Only.

Uprosertib (GSK2141795) is a potent, selective, ATP-competitive and orally bioavailable AKT inhibitor with IC50 of 0.066 nM, 1.4 nM and 1.5 nM for Akt1, Akt2 and Akt3 respectively.

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5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1880 In stock
50 mg ￥2980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Uprosertib (GSK2141795) is a potent, selective, ATP-competitive and orally bioavailable AKT inhibitor with IC50 of 0.066 nM, 1.4 nM and 1.5 nM for Akt1, Akt2 and Akt3 respectively.
Uprosertib (GSK2141795) inhibits the kinase activity of the E17K AKT 1 mutant protein with EC50 of 0.2 nM.
Uprosertib (GSK2141795) showes concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both cell lines, exhibits growth inhibition in human cancer cell lines.
Uprosertib (GSK2141795) (10, 20 and 30 mg/kg, QD) shows tumor growth inhibition (TGI) of 73, 85 or 93% in mice bearing BT474 tumors.
Combining Uprosertib (GSK2141795) with the AKT inhibitor or MEK inhibitor (GSK2110212; trametinib) resulted in an enhanced anti-tumor effect accompanied with greater reduction in phospho-S6 levels.

物理化学性质&存储条件

分子量 429.25
分子式 C18H16Cl2F2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(1-Amino-3-(3,4-difluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide

参考文献

1. Datta J, et al. Mol Cancer Ther. 2017 Apr;16(4):614-624.

2. Dumble M, et al. PLoS One. 2014 Jun 30;9(6):e100880.

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