BAY-876

SKU: orb1225893

Description

A potent, highly selective and oral bioavailable GLUT1 inhibitor with IC50 of 2 nM; displays >100-fold selectivity against GLUT2, GLUT3, and GLUT4; exhibits good metabolic stability in vitro and high oral bioavailability in vivo.

Key Properties

• CAS Number: 1799753-84-6
• MW: 496.4164
• Purity: >98% (HPLC)
• Formula: C₂₄H₁₆F₄N₆O₂
• SMILES: O=C(C1=NC2=CC(F)=CC=C2C(C(NC3=C(C)N(CC4=CC=C(C=C4)C#N)N=C3C(F)(F)F)=O)=C1)N
• Target: GLUT
• Solubility: DMSO: ≥ 100 mg/mL

Bioactivity

• In Vivo:
  Animal model: Female NOD-scid IL2rgnull (NSG) mice carrying SKOV-3 subcutaneous (s. c.) xenografts. Dosage: 1.5, 3, 4.5 mg/kg. Administration: Oral administration; daily; for 28 days. Result: Caused a clear dose-dependent inhibition of tumorigenicity.
• In Vitro:
  Cell Proliferation Assay Cell line: SKOV-3 and OVCAR-3 cells. Concentration: 25, 50, 75 nM. Incubation time: 24 and 72 hours. Result: Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAY876

Quick Database Links

Gene Symbol

GLUT