For research use only. Not for therapeutic Use.
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[1]. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth[2].
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[2].
BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice[2].
Catalog Number | I002338 |
CAS Number | 1799753-84-6 |
Synonyms | 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide |
Molecular Formula | C24H16F4N6O2 |
Purity | ≥95% |
InChI | InChI=1S/C24H16F4N6O2/c1-12-20(21(24(26,27)28)33-34(12)11-14-4-2-13(10-29)3-5-14)32-23(36)17-9-19(22(30)35)31-18-8-15(25)6-7-16(17)18/h2-9H,11H2,1H3,(H2,30,35)(H,32,36) |
InChIKey | BKLJDIJJOOQUFG-UHFFFAOYSA-N |
SMILES | CC1=C(C(=NN1CC2=CC=C(C=C2)C#N)C(F)(F)F)NC(=O)C3=CC(=NC4=C3C=CC(=C4)F)C(=O)N |
Reference | [1]. Siebeneicher H et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Aug 23. [2]. Ma Y, et al. Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876. Cancers (Basel). 2018 Dec 31;11(1). |