Molecular Formula | C24H16F4N6O2 |
Molar Mass | 496.4164 |
Melting Point | >250oC (dec.) |
Solubility | DMSO: ≥ 100 mg/mL |
Appearance | Morphological powder |
Color | white to beige |
Storage Condition | 2-8°C |
Physical and Chemical Properties | Bioactive BAY-876 is an effective and selective GLUT1 inhibitor (IC50=0.002 μM), and its selectivity for GLUT1 is 100 times higher than that for GLUT2, GLUT3 and GLUT4. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.014 ml | 10.072 ml | 20.144 ml |
5 mM | 0.403 ml | 2.014 ml | 4.029 ml |
10 mM | 0.201 ml | 1.007 ml | 2.014 ml |
5 mM | 0.04 ml | 0.201 ml | 0.403 ml |
Target
Target Value
GLUT1
(Cell-free assay) 0.002 μM
in vitro studies
BAY-876 is an inhibitor with high selectivity to GLUT1, and its selectivity is 4700, 800 and 135 times to GLUT2, GLUT3 and GLUT4 respectively.
In vivo studies
BAY-876 has a low clearance rate in rats and dogs. Its volume of distribution is moderate, with a half-life of 2.5 hours in rats and 22 hours in dogs. The oral bioavailability (F%) in rats and dogs was 85% and 79%, respectively. BAY-876 has good in vivo pharmacokinetics (high oral bioavailability and long half-life), making it a chemical probe marker with great potential for targeting GLUT1 inhibitors in cancer treatment.