GSK2636771
Selective PI3Kß inhibitor / GSK2636771 is a potent, selective (>1000-fold over α, 10-fold over δ, and >2000-fold over γ), and orally bioavailable inhibitor of PI3Kß (IC50 = 5.2 nM).1 Active in vitro against multiple types of PTEN-deficient cancer cells. GSK2636771 potently blocked migration and invasion of DU145 prostate cancer cells.2 GSK2636771 has also been identified as a GPR39 agonist.3
Biochemicals & reagents
1372540-25-4
1) Mateo et al. (2017), A First-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors; Clin. Cancer Res. 23 5981 2) Zhang et al. (2018), Phosphatidylinositol 3-kinase ß and ? isoforms play key roles in metastasis of prostate cancer DU145 cells; FASEB J. 32 5967 3) Sato et al. (2016); Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc, Mol. Pharmacol., 90 726
-20°C
TARGET: Kinase; GPCR -- DISEASE AREA: Cancer