BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
IC50&Target
GLUT1
2 nM (IC50)
GLUT2
10.08 μM (IC50)
GLUT3
1.67 μM (IC50)
GLUT4
0.29 μM (IC50)
体外研究
BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.
Cell Proliferation Assay
Cell Line:
SKOV-3 and OVCAR-3 cells
Concentration:
25, 50, 75 nM
Incubation Time:
24 and 72 hours
Result:
Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.
体内研究
BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice.