GSK1059615是一种PI3Kα/β/δ/γ (可逆的)和mTOR的双重抑制剂，IC50分别为0.4 nM/0.6 nM/2 nM/5 nM和12 nM。GSK1059615也抑制mTOR，IC50为12 nM。GSK1059615抑制PI3K通路，诱导细胞停滞在G1期，可观察到凋亡。GSK1059615有效作用于胸腺癌细胞。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

GSK 1059615; GSK-1059615

Powder

DMSO ：2mg/ml(6 mM)

PI3Kα ,PI3Kβ ,PI3Kδ ,PI3Kγ ,mTOR

The pyridinylquinoline derivative GSK1059615 is a novel, ATP-competitive, and reversible inhibitor of the class I family of PI3Ks. GSK1059615 inhibits PI3K signaling, induces G1 arrest and apoptosis, especially in breast tumor cells. Data summarized in another review also shows that GSK1059615 inhibits PI3Kα, β, γ and δ, with Ki of 0.42 nM, 0.6 nM, 0.47 nM and 1.7 nM, respectively. Another report shows that GSK1059615 inhibits PI3Kα with IC50 of 2 nM. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC50 of 40 nM.

In xenograft mice models of BT474 or HCC1954 breast cancer cells, GSK1059615 (25 mg/kg) effectively inhibits tumor growth.