AZD3965

Catalog No.S7339 Batch:S733904

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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
* <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.)

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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 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 23 publications

Deciphering metabolic heterogeneity in retinoblastoma unravels the role of monocarboxylate transporter 1 in tumor progression [ Biomark Res, 2024, 12(1):48] PubMed: 38730450
H3K9 lactylation in malignant cells facilitates CD8+ T cell dysfunction and poor immunotherapy response [ Cell Rep, 2024, 43(9):114686] PubMed: 39216002
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
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

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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.