AZD3965

Catalog No.S7339

For research use only.

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

CAS No. 1448671-31-5

Selleck's AZD3965 has been cited by 10 Publications

1 Customer Review

Purity & Quality Control

Choose Selective MCT Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Raji MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MknZO|IhcA>? MVvHTVUxRTF{LkO1JI5O NWrYRmZPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwOVAyQTlpPkK5NFUxOTl7PD;hQi=>
WSU-DLCL-2 NWP5cHBwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3q4XFczKGh? NHzCNIdIUTVyPU[uNVEhdk1? NHjqXWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUC1NFE6QSd-MkmwOVAyQTl:L3G+
SU-DHL-10 M3n2XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHTJS2g4OiCq M1rQXWdKPTB;ND6yNkBvVQ>? MonhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlyNUCxPVkoRjJ7MEWwNVk6RC:jPh?=
Karpas-422 NVPweHJiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYe3NkBp Mn7ZS2k2OD1|OUWuN|ghdk1? NG\yWGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUC1NFE6QSd-MkmwOVAyQTl:L3G+
Hut78 NEPSXY1HfW6ldHnvckBie3OjeR?= NGXHemU2NCB{NTygOVAxKG6P M2TqeFI1KGh? M1vFdVI1cCCneIDvd5Vz\SC2bzDhJIxwfyClb37j[Y51emG2aX;uJI9nKEGcREO5OlUhMDWwTTmgcIVlKHSxIHGgNVAu\m:uZDDieYlt\C23cDDpckBN[WO2YYTlTUBqdiCPQ2S0L{BJfXR5ODDoeY1idiCueX3wbI9u[SClZXzsd{whf2irY3ige4F{KHO3c4ThbY5m\CCjdDDobYdp\XJiZIL1[{Bkd26lZX70doF1cW:wczCoNlVvVSCjbnSgOVAxdk1r NGDwbXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmyN|g3OSd-Mki5NlM5PjF:L3G+
HT29 MkXhSpVv[3Srb36gZZN{[Xl? MXm1MEAzPSxiNUCwJI5O NVLZd5IzOjRiaB?= NHiyb|VE\WyuczDzbI94\WRiYTD0doVv\CC2b4fhdoR{KGGwIHnuZ5Jm[XOnIHnuJGxi[3SjdHXJJJJmdGG2aY\lJJRwKGOxboTyc4x{KHerdHigOY5OKGGwZDCyOY5OKEGcREO5OlUhf2irY3igc45tgSCkZXPhcYUhe2mpbnnmbYNidnRid3n0bEBmgHCxc4Xy[UB1dyB3MECgcm0hSVqGM{m2OUBz\WGlaHnu[{B2eCC2bzC0MYZwdGRuIILlcIF1cX[nIITvJINwdnS{b3zzMi=> M1HKV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUKzPFYyLz5{OEmyN|g3OTxxYU6=
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 29050199
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 (from reference)

Animal Research:[2]
  • Animal Models: Nonobese diabetic scid-γ mice bearing COR-L103 xenografts
  • Dosages: 100 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 515.51
Formula

C21H24F3N5O5S

CAS No. 1448671-31-5
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01791595 Completed Drug: AZD3965 Adult Solid Tumor|Diffuse Large B Cell Lymphoma|Burkitt Lymphoma Cancer Research UK February 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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