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AZD3965

Catalog No. T3210 CAS 1448671-31-5

Synonyms: AZD 3965, AZD-3965

AZD3965 (AZD-3965) is a selective inhibitor of monocarboxylate transporter 1 (MCT1).

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AZD3965, CAS 1448671-31-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
2 mg	In stock	$ 72.00
5 mg	In stock	$ 119.00
10 mg	In stock	$ 148.00
50 mg	In stock	$ 449.00
1 mL * 10 mM (in DMSO)	In stock	$ 135.00

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Purity: 99.85%

Purity: 99.75%

Purity: 99.71%

Purity: 99.35%

Purity: 98.99%

Purity: 98.81%

Purity: 98.03%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD3965 (AZD-3965) is a selective inhibitor of monocarboxylate transporter 1 (MCT1).
Targets&IC50	MCT1:1.6 nM (Ki)
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]
Kinase Assay	Cells are plated overnight and treated with 100 nM AZD3965 or vehicle for 24 hours. The cells are then washed, once in PBS and twice with lysis buffer (50 mM Mops, 100 mM KCl, 5 mM MgCl2, 1 mM EDTA, 0.1 mM DTT, 1 mM PMSF supplemented with 1× mini complete protease inhibitor cocktail tablets. The cells are harvested by scraping and centrifugation, and the pellet snap frozen without buffer in liquid nitrogen. Frozen aliquots of cells are thawed on ice and re-suspended in lysis buffer. Cells are lysed by 3 rounds of freezing in liquid nitrogen and thawing at 37°C for 2 minutes each. Lysates are subsequently centrifuged (13000 g, 10min, 4°C) until clear and then stored on ice. Enzyme activity in the cell lysates is determined using a micro-plate reader to measure either production or depletion of NADH/NADPH, through its absorbance at 340/10 nm, occurring as a result of direct or coupled enzyme reactions. The 96 well plates used for the assays are pre-heated to 37°C for 10 minutes prior to starting reactions, initiated by the addition of 5 μL cell lysate to 95 μL of reaction buffer (50 mM Mops pH 7.4, 100 mM KCl, 5 mM free magnesium). The standard reaction buffer is supplemented to assay the kinetics of the different enzymes. Absorbance values for controls are subtracted from absorbance of corresponding reactions. Graphpad prism 6 is used to plot V0 values against substrate concentration and determine Vmax and Km values. The Vmax is then normalised to the protein concentration in the cell lysate[1].

Synonyms	AZD 3965, AZD-3965
Molecular Weight	515.51
Formula	C21H24F3N5O5S
CAS No.	1448671-31-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 100 mg/mL (193.98 mM)

DMSO: 100 mg/mL (193.98 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Critchlow SE, et al. 2012. AACR 103rd Annual Meeting. 2. Polański R, et al. Clin Cancer Res. 2014, 20(4), 926-937. 3. Bola BM, et al. Mol Cancer Ther. 2014, 13(12), 2805-2816.

Citations

1. Li F F, Zhang Y L, Guo D X, et al. Biochemometric approach combined with 1D CSSF-TOCSY for the identification of sensitization agents in Curcuma longa L. and prediction of their action mechanisms. Microchemical Journal. 2022 October 2. Li X, Zhang Y, Xu L, et al.Ultrasensitive sensors reveal the spatiotemporal landscape of lactate metabolism in physiology and disease.Cell Metabolism.2023, 35(1): 200-211. e9. 3. Zhang Y T, Xing M L, Fang H H, et al.Effects of lactate on metabolism and differentiation of CD4+T cells.Molecular Immunology.2023, 154: 96-107.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Ion Channel Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Preclinical Compound Library Anti-Cancer Compound Library

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Related compounds with same targets

7ACC1 Niflumic acid α-Cyano-4-hydroxycinnamic acid Lactate transportor 1 AR-C155858 AZD0095 MCT1-IN-3 VB124

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AZD3965 1448671-31-5 Membrane transporter/Ion channel Monocarboxylate transporter inhibit Inhibitor Monocarboxylate Transporter AZD 3965 AZD-3965 inhibitor

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