化合物GSK-2636771 T2073
面议
- TargetMol
- 生产商
- 进口
- 美国
- 现货
- 全国
- 8
- 0
Product IntroductionBioactivity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
AI问答
配套的仪器设备？
可以搭配的相关耗材试剂？
耗材描述
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
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
猜你喜欢
感兴趣产品