化合物GSK-2636771 T2073

Product Introduction
Bioactivity


英文名: GSK2636771

描述: GSK2636771 是选择性的、口服有效的PI3Kβ抑制剂，Ki=0.89 nM，IC50=5.2 nM，比p110α和p110γ的选择性高900倍，比p110δ同种型的选择性高10倍。

细胞实验: Cells are plated in 96-well microtiter plates at densities ranging from 1,500 to 15,000 cells/well, optimized for untreated control cells to be 80-90% confluent at the endpoint of the experiment. After 24 h, cells are treated with serial dilutions (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). At least three independent experiments in triplicate per cell line targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test (GraphPad Prism), and a two-tailed P value <0.05 is considered statistically significant. (Only for Reference)

体外活性: 在小鼠中,GSK-2636771 （100 mg/kg）不增加葡萄糖/胰岛素水平.在移植瘤模型中,GSK-2636771降低磷酸化的蛋白激酶Akt（Ser473）水平.

体内活性: 在PTEN缺失细胞系中,GSK-2636771具有特异的抑制活性,在人前列腺癌PC-3（EC50=36 nM）和乳腺癌HCC70（EC50=72 nM）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 27 mg/mL (62.3 mM)


关键字: Inhibitor | PI3K | Phosphoinositide 3-kinase | inhibit | GSK2636771

相关产品: mTOR inhibitor 9e | Bufarenogin | Hirsutenone | IHMT-PI3Kδ-372 S-isomer | LX2343 | Inavolisib | PI3Kγ inhibitor 1 | 740 Y-P | Fimepinostat | CHMFL-PI3KD-317

相关库: Antioxidant Compound Library | Drug Repurposing Compound Library | Glycometabolism Compound Library | Anti-Cancer Drug Library | Neural Regeneration Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途