Chemical Name: N4-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoro-2,4-quinolinedicarboxamide
Biological ActivityPotent and selective GLUT1 inhibitor (IC50 = 2 nM). Displays selectivity for GLUT1 over GLUT2/3/4 (IC50 values are 10.8, 1.67 and 0.29 μM, respectively). Induces cell death in hypoxic conditions in vitro. Inhibits glucose uptake by Hela-MaTu cells. Cell permeable and orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Identification and optimization of the first highly selective GLUT1 inhibitor BAY-876.
Siebeneicher et al.
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