PI 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation. Its signaling pathway is the most commonly mutated pathway in human cancers. GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM) and the common activating mutants of p110α (E542K, E545K, and H1047R) found in cancer. It prevents proliferation in BT474 tumor xenografts and reduces MAPK signaling following twice daily dosing at 25 mg/kg.
![5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione](https://www.chemicalbook.com/CAS/GIF/958852-01-2.gif)
