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。

GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm.

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.

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）。

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)

1372540-25-4

C22H22F3N3O3

433.42

GSK 2636771;GSK-2636771;GSK2636771

H2O:<1 mgml
DMSO:27 mg/mL (62.3 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years