AZD3965

SKU: orb1304420

Description

AZD3965 is a potent and selective small molecule inhibitor of monocarboxylate transporter 1 (MCT1). It is utilized in cancer metabolism research to investigate tumor glycolysis and has demonstrated anti-tumor activity in both cellular assays and in vivo xenograft models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1448671-31-5
• MW: 515.51
• Purity: 99.87%
• Formula: C₂₁H₂₄F₃N₅O₅S
• SMILES: CC(C)n1c2sc(Cc3c(C)[nH]nc3C(F)(F)F)c(C(=O)N3C[C@](C)(O)CO3)c2c(=O)n(C)c1=O
• Target: Monocarboxylate transporter
• Solubility: DMSO:100 mg/mL (193.98 mM);Ethanol:100 mg/mL (193.98 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.76 mM)

Bioactivity

• Target IC50:
  MCT1:1.6 nM (Ki)
• In Vivo:
  In nonobese diabetic scid-γ mice bearing COR-L103 xenografts, AZD3965 (100 mg/kg, p.o.) reduces tumor growth and increased intratumor lactate. In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity.
• In Vitro:
  In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD 3965, AZD3965, AZD-3965, Inhibitor, MCT1, inhibit, Monocarboxylate Transporter, Monocarboxylate transporter, Monocarboxylatetransporter

Compound Identifiers

PubChem CID

10369242