BAY-876

Description: BAY-876 is a potent and highly-selective GLUT1 inhibitor with IC50 of 0.002 uM and with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively. BAY-876 exhibited good metabolic stability in?vitro and high oral bioavailability in?vivo. GLUT1 overexpression has been reported in many types of human cancers, including those of brain, 6 breast, colon, kidney, lung, ovary, and prostate, and is correlated with advanced cancer stages and poor clinical outcomes. Despite the long-known fact that the facilitative glucose transporter GLUT1 is one of the key players safeguarding the increase in glucose consumption of many tumor entities even under conditions of normal oxygen supply (known as the Warburg effect), only few endeavors have been undertaken to find a GLUT1-selective small-molecule inhibitor.

References: ChemMedChem. 2016 Oct 19; 11(20):2261-2271.

Related CAS#:1799759-24-2 ( BAY-588)