GSK1059615,958852-01-2

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YZ剂描述：

产品名称：GSK1059615

产品别名：(5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione

英文别名：GSK 1059615;GSK-1059615

靶点：PI3Kα ,PI3Kβ ,PI3Kδ ,PI3Kγ ,mTOR

CAS：958852-01-2

纯度：>98%

外观：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

GSK1059615是一种PI3Kα/β/δ/γ (可逆的)和mTOR的双重YZ剂，IC50分别为0.4 nM/0.6 nM/2 nM/5 nM和12 nM。GSK1059615也YZmTOR，IC50为12 nM。GSK1059615YZPI3K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。

溶解性：DMSO ：2mg/ml(6 mM)

体外研究：

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.

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

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