GSK 1059615, a pyridinylquinoline derivative, is a novel, ATP-competitive, and reversible class I PI 3-kinase inhibitor. GSK 1059615 inhibits PI 3-kinase signaling and induces G1 arrest and apoptosis, especially in breast tumor cells. GSK 1059615 inhibits PI 3-kinase α (IC50 of 2 nM, Ki of 0.42 nM), β (Ki of 0.6 nM), γ (Ki of 0.47 nM) and δ (Ki of 1.7 nM). GSK 1059615 is also an inhibitor of mTOR (FRAP) (IC50 of 0.4-12 nM).
Soluble in DMSO (10 mM), DMSO:PBS(pH 7.2) 1:1 (0.5 mg/ml), water (<1 mg/ml), ethanol (<1 mg/ml), and DMF (0.25 mg/ml).
Store at 4° C
1.44 g/cm3 (Predicted)
n20D 1.76 (Predicted)
PI3Kα: IC50 = 0.4 nM; PI3Kβ: IC50 = 0.6 nM; PI3Kδ: IC50 = 2 nM; PI3Kγ: IC50 = 5 nM; mTOR: IC50 = 12 nM; Inhibits the phosphorylation of Akt at S473: IC50 = 40 nM (T47D and BT474 cancer cells)
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