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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-GSK2636771
GSK2636771

Chemical Structure : GSK2636771

CAS No.: 1372540-25-4

GSK2636771 (GSK 2636771)

货号: PC-21944Not For Human Use, Lab Use Only.

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with Ki/IC50 of 0.89/5.2 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with Ki/IC50 of 0.89/5.2 nM, respectively.
GSK2636771 displays 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
GSK2636771 causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells.
GSK2636771 decreases AKT phosphorylation in prostate and breast cancer cell lines, suppresses cell and tumor growth in vivo.

物理化学性质&存储条件

分子量 433.43
分子式 C22H22F3N3O3
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

2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid

参考文献

1. Weigelt B, et al. Clin Cancer Res. 2013 Jul 1;19(13):3533-44.

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