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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification and optimization of the first highly selective GLUT1 inhibitor BAY-876.
Siebeneicher et al.
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