Name | BAY-876 |
Description | BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth. |
In vitro | METHODS: HNSCC cell lines SCC47 and RPMI2650 were treated with BAY-876 (0.01-100 µM) for 24 h. Cell viability was detected by crystal violet staining.
RESULTS: After 24 h, BAY-876 reduced the viable SCC47 and RPMI2650 cells. [1]
METHODS: Ovarian cancer cells SKOV-3, OVCAR-3 and HEY were treated with BAY-876 (25-75 nM) for 24 h. The rate of glycolysis was detected by Glycolysis Assay.
RESULTS: Incubation with BAY-876 dose-dependently decreased the rate of glycolysis in SKOV-3, OVCAR-3 and HEY cells. Although this anti-glycolytic effect of BAY-876 was detectable at single-digit nanomolar concentrations, half-maximal inhibition was achieved at 25-50 nM of the compound. [2] |
In vivo | METHODS: To detect the antitumor activity in vivo, BAY-876 (1.5-4.5 mg/kg, 0.5% hydroxypropyl methyl cellulose and 0.1% Tween 80) was administered by gavage to NSG mice bearing SKOV-3 xenografts once a day for four weeks.
RESULTS: BAY-876 showed a significant dose-dependent inhibitory effect on tumorigenicity. The maximum effect was observed in the 4.5 mg/kg/day treatment group. After 2 weeks of treatment, tumors were significantly reduced. At the endpoint, final mean tumor volume and tumor weight decreased by 68% and 66%, respectively, compared to the excipient control group. However, the dose of 4.5 mg/kg/day was toxic to NSG mice. [2] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 3 mg/mL (6.04 mM) DMSO : 15 mg/mL (30.23 mM), Sonication is recommended.
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Keywords | Inhibitor | metabolism | transporter | ovarian | glycolytic | cancer | BAY-876 | Glucose transporter | BAY 876 | glucose | inhibit | BAY876 | orally | GLUT |
Inhibitors Related | MSNBA | Fraxin | LDN-212320 | Venuloside A | Brilliant Yellow | WAY-213613 hydrochloride | Jujuboside A | IPN60090 | SLC26A3-IN-1 | Phloretin | GT 949 | Telaglenastat |
Related Compound Libraries | Highly Selective Inhibitor Library | Glycometabolism Compound Library | Bioactive Compound Library | Glutamine Metabolism Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Cancer Active Compound Library |