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AZD3965 MCT1 Inhibitor

Name: AZD3965
Brand: Selleck Chemicals
SKU: S7339
Availability: InStock
Rating: 5 (29 reviews)

Cat.No.S7339

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.

Chemical Structure

Molecular Weight: 515.51

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor ATPase TRP Channel GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel Amino acid transporter GLUT CRM1 VDAC BCRP NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	515.51	Formula	C₂₁H₂₄F₃N₅O₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1448671-31-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (19.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	MCT1 ^[1]
In vitro	In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. ^[1] This compound inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. ^[2] In H526, HGC27 cells and DMS114 cells, this chemical 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, this compound (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity. ^[3]
References	http://cancerres.aacrjournals.org/content/72/8_Supplement/3224 https://pubmed.ncbi.nlm.nih.gov/24277449/ https://pubmed.ncbi.nlm.nih.gov/25281618/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		29050199

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

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