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GSK2636771

CAS No. : 1372540-25-4

MCE 站：GSK2636771

产品活性：GSK2636771 是一种口服有效的选择性 PI3Kβ 抑制剂，K_i和IC₅₀分别为0.89，5.2 nM，比p110α和p110γ的选择性高900倍，比p110δ同种型的选择性高10倍。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: GSK2636771 treatment 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. Inhibition of p110β by GSK2636771 or AZD6482 leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines, whereas only marginal effects on AKT activation are observed in EEC cells.

In Vivo: GSK2636771 is a p110β inhibitor, and the p110β primes cells for response to growth factor stimulation. While p110β inhibition suppresses cell and tumor growth, dual targeting of p110α/β enhances apoptosis and provides sustained tumor response in mice model.

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