AZD3965

Catalog No.S7339 Batch:S733907

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Technical Data

Formula

C21H24F3N5O5S
Molecular Weight 515.51 CAS No. 1448671-31-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (193.98 mM)
Ethanol 100 mg/mL (193.98 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml 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. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[3]
  • 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.
Animal Study:

[2]
  • Animal Models

    Nonobese diabetic scid-γ mice bearing COR-L103 xenografts

  • Dosages

    100 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Cancer Res, 2017, 77(20):5591-5601]

Selleck's AZD3965 has been cited by 20 publications

Lactate promotes myogenesis via activating H3K9 lactylation-dependent up-regulation of Neu2 expression [ J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363] PubMed: 37919243
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546] PubMed: 37428012
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546] PubMed: 37428012
Functional heterogeneity of MCT1 and MCT4 in metabolic reprogramming affects osteosarcoma growth and metastasis [ J Orthop Surg Res, 2023, 18(1):131] PubMed: 36814318
The lactate-NAD+ axis activates cancer-associated fibroblasts by downregulating p62 [ Cell Rep, 2022, 39(6):110792] PubMed: 35545049
Succinate uptake by T cells suppresses their effector function via inhibition of mitochondrial glucose oxidation [ Cell Rep, 2022, 40(7):111193] PubMed: 35977513
A Heme-Binding Transcription Factor BACH1 Regulates Lactate Catabolism Suggesting a Combined Therapy for Triple-Negative Breast Cancer [ Cells, 2022, 11(7)1177] PubMed: 35406740
Metabolic heterogeneity protects metastatic mucosal melanomas cells from ferroptosis [ Int J Mol Med, 2022, 50(4)124] PubMed: 36004461
PFKFB4 promotes angiogenesis via IL-6/STAT5A/P-STAT5 signaling in breast cancer [ J Cancer, 2022, 13(1):212-224] PubMed: 34976184
Construction and Functional Evaluation of a Three-Dimensional Blood-Brain Barrier Model Equipped With Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells [ Pharm Res, 2022, 39(7):1535-1547] PubMed: 35411503

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.