MSC-4381

SKU: orb1692555

Description

MSC-4381 (MCT4-IN-1) is a potent, selective, and orally bioavailable inhibitor of the monocarboxylate transporter 4 (MCT4/SLC16A3). It is a research tool for investigating cancer metabolism, with applications in in vitro and in vivo studies of osteosarcoma and other hypoxic tumors.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2445185-57-7
• MW: 537.97
• Purity: 99.55% (May vary between batches)
• Formula: C₂₆H₂₀ClN₃O₆S
• SMILES: CCOc1ccc(c2ncccc12)S(=O)(=O)Nc1ccc(Cl)cc1C#Cc1cnc(cc1OC)C(O)=O
• Target: Monocarboxylate transporter
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (4.65 mM);DMSO:50 mg/mL (92.94 mM)

Bioactivity

• In Vivo:
  When MCT4-IN-1 (30 mg/kg; oral; single dose) was used only in combination with MCT1/2 inhibitors, lactic acid accumulation in tumor cells was significant; MCT4-IN-1 (30 mg/kg/day; for 15 consecutive days) had no significant antitumor activity; MCT4-IN-1 (0.2 mg/kg; intravenous injection) had a T1/2 of 1 hour, a CL of 0.33 L/hkg, a Cmax of 489 ng/mL, and a Vss of 0.4 L/kg in mice.
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• In Vitro:
  MCT4-IN-1 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC50 of 1 nM. On-target activity was confirmed by fluorescence cross correlation spectroscopy (FCCS) with a Ki of 11 nM.
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Storage & Handling

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

Alternative Names

MSC 4381, MSC4381, MCT4, MCT-4-IN-1, MCT4-IN-1, MCT4 IN 1, MCT4IN1, Monocarboxylate transporter, Monocarboxylatetransporter

Compound Identifiers

PubChem CID

150189198