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 12 Publications

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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 MmXrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXzOb3dtPzJiaB?= MV;HTVUxRTF{LkO1JI5O NGHhdYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUC1NFE6QSd-MkmwOVAyQTl:L3G+
WSU-DLCL-2 MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWK3NkBp M2DYeWdKPTB;Nj6xNUBvVQ>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTB3MEG5PUc,OjlyNUCxPVk9N2F-
SU-DHL-10 NFj3Om1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHq5ZlE4OiCq NYLMeXB5T0l3ME20MlIzKG6P NEfwZWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUC1NFE6QSd-MkmwOVAyQTl:L3G+
Karpas-422 NV\OcnRrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYi3NkBp MmH1S2k2OD1|OUWuN|ghdk1? NVnUZZJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwOVAyQTlpPkK5NFUxOTl7PD;hQi=>
Hut78 NIDZeZZHfW6ldHnvckBie3OjeR?= M4DmPFUtKDJ3LDC1NFAhdk1? NXf6RoMzOjRiaB?= NXPEN5p[OjSqIHX4dI9{fXKnIITvJIEhdG:5IHPvcoNmdnS{YYTpc44hd2ZiQWrEN|k3PSBqNX7NLUBt\WRidH:gZUAyOC2ob3zkJIJ2cWymLYXwJIlvKEyjY4TheIVKKGmwIF3DWFQsKEi3dEe4JIh2dWGwIHz5cZBpd22jIHPlcIx{NCC5aHnjbEB4[XNic4XzeIFqdmWmIHH0JIhq\2incjDkdpVoKGOxbnPlcpRz[XSrb37zJEgzPW6PIHHu[EA2ODCwTTm= NFfnZlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmyN|g3OSd-Mki5NlM5PjF:L3G+
HT29 MVXGeY5kfGmxbjDhd5NigQ>? MVy1MEAzPSxiNUCwJI5O M4PyT|I1KGh? M4nqZmNmdGy|IIPoc5dm\CCjIITy[Y5lKHSxd3Hy[JMh[W5iaX7jdoVie2ViaX6gUIFkfGG2ZVmgdoVt[XSrdnWgeI8h[2:wdILvcJMhf2m2aDC1cm0h[W6mIEK1cm0hSVqGM{m2OUB4cGmlaDDvcox6KGKnY3Ht[UB{cWewaX\pZ4FvfCC5aYToJIV5eG:|dYLlJJRwKDVyMDDuUUBCYkR|OU[1JJJm[WOqaX7nJJVxKHSxIESt[o9t\CxicnXsZZRqfmVidH:gZ49vfHKxbIOu M1\tPFxiKHSjcnfleF0oZ2KuYX7rK{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

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)

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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
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Molarity Calculator

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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|AstraZeneca April 23 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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