Home Transmembrane Transporters MCT inhibitor AZD3965 For research use only.

AZD3965

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.

AZD3965 Chemical Structure

AZD3965 Chemical Structure

CAS No. 1448671-31-5

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AZD3965 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Raji Growth inhibition assay 72 h GI50=12.35 nM 29050199
WSU-DLCL-2 Growth inhibition assay 72 h GI50=6.11 nM 29050199
SU-DHL-10 Growth inhibition assay 72 h GI50=4.22 nM 29050199
Karpas-422 Growth inhibition assay 72 h GI50=395.38 nM 29050199
Hut78 Function assay 5, 25, 500 nM 24 h 24h exposure to a low concentration of AZD3965 (5nM) led to a 10-fold build-up in LactateI in MCT4+ Hut78 human lymphoma cells, which was sustained at higher drug concentrations (25nM and 500nM) 28923861
HT29 Function assay 5, 25, 500 nM 24 h Cells showed a trend towards an increase in LactateI relative to controls with 5nM and 25nM AZD3965 which only became significant with exposure to 500 nM AZD3965 reaching up to 4-fold, relative to controls. 28923861
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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 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]
Cell Research Cell lines DMS114, H526 and HGC27 cells
Concentrations 1.6 nM
Incubation Time 24 h
Method

Cells were incubated in either normoxia, 1% oxygen (hypoxia) or anoxia in complete media supplemented with AZD3965 or DMSO vehicle for 24 hours.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 29050199
In Vivo
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]
Animal Research Animal Models Nonobese diabetic scid-γ mice bearing COR-L103 xenografts
Dosages 100 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01791595 Completed
Adult Solid Tumor|Diffuse Large B Cell Lymphoma|Burkitt Lymphoma
Cancer Research UK|AstraZeneca
 April 23 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 515.51 Formula

C21H24F3N5O5S
CAS No. 1448671-31-5 SDF Download AZD3965 SDF
Smiles CC1=C(C(=NN1)C(F)(F)F)CC2=C(C3=C(S2)N(C(=O)N(C3=O)C)C(C)C)C(=O)N4CC(CO4)(C)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (193.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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