AZD3965

Catalog No.S7339

AZD3965 Chemical Structure

Molecular Weight(MW): 515.51

AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.

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Biological Activity

Description AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.
Targets
MCT1 [1]
In vitro

In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. [1] AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. [2] In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake. [3]

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. [2] In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity. [3]

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: Nonobese diabetic scid-γ mice bearing COR-L103 xenografts
  • Formulation: 0.5% hydroxypropyl methyl cellulose, 0.1% tween 80
  • Dosages: 100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (193.98 mM)
Ethanol 100 mg/mL (193.98 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 515.51
Formula

C21H24F3N5O5S

CAS No. 1448671-31-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01791595 Recruiting Adult Solid Tumor|Diffuse Large B Cell Lymphoma|Burkitt Lymphoma Cancer Research UK February 2013 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID