BAY-876

SKU: orb1303859

Description

BAY-876 is a potent and selective oral inhibitor of the glucose transporter GLUT1 (IC50=2 nM), showing over 100-fold selectivity versus GLUT2/3/4. It suppresses glycolytic metabolism and demonstrates antitumor activity in both cellular assays and in vivo models, making it a valuable tool for cancer metabolism research.

Research Area

Cell Biology, Immunology & Inflammation

Key Properties

• CAS Number: 1799753-84-6
• MW: 496.4
• Purity: >98%
• Formula: C₂₄H₁₆F₄N₆O₂
• SMILES: Cc1c(NC(=O)c2cc(nc3cc(F)ccc23)C(N)=O)c(nn1Cc1ccc(cc1)C#N)C(F)(F)F
• Target: Glucose transporter
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  GLUT4:0.29 μM|T24 cells:24.31 μM|GLUT3:1.67 μM|786-O cells:53.56 μM|GLUT1:0.002 μM|GLUT1:2 nM|5637 cells:21.62 μM|EJ cells:18.72 μM|GLUT2:10.08 μM
• 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.
• 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. 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

4-N-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide

Compound Identifiers

PubChem CID

118191391