AZD3965 (AZD-3965, AZD 3965)

For research purposes only

Cat. No BA27112015

Availability In Stock

Description of biological activity

AZD3965 is a selective inhibitor of MCT1 with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited by AZD3965 in lymphoma cell lines that preferentially express MCT1. It is currently undergoing phase I clinical trial in patients with advanced solid tumors or lymphoma [1,2]

Therapeutic area

Cancer, auto-immune.

Biological target category

Monocarboxylate transporter.

TECHNICAL INFORMATION

5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione Selective inhibitor of MCT1 with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited.

IUPAC Name: 5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione

Chemical Formula: C21H24F3N5O5S

SMILES: CC(C)N1C(=O)N(C)C(=O)C=2C(C(=O)N3C[C@](C)(O)CO3)=C(CC4=C(C)NN=C4C(F)(F)F)SC12

CAS Number: 733809-45-5; 1448671-31-5

Molecular Weight: 515.510

Purity: >98%

Appearance: Pale yellow powder

Solubility: DMSO

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light.

Stability: Stable under normal condition.

Shipping Conditions: Shipped at room temperature.

USE PROTOCOL

Soluble in DMSO. If precipitate is observed, vortex for 5 minutes.

REFERENCES

1. Carlotta Granchi, Daniele Fancelli, Filippo Minutolo, An update on therapeutic opportunities offered by cancer glycolytic metabolism, Bioorganic & Medicinal Chemistry Letters, Volume 24, Issue 21, 1 November 2014, Pages 4915-4925, ISSN 0960-894X, http://dx.doi.org/10.1016/j.bmcl.2014.09.041. (http://www.sciencedirect.com/science/article/pii/S0960894X14009834)

2. Abstract 3224: Pre-clinical targeting of the metabolic phenotype of lymphoma by AZD3965, a selective inhibitor of monocarboxylate transporter 1 (MCT1) Susan E. Critchlow, Lorna Hopcroft, Lorraine Mooney, Nicola Curtis, Nicky Whalley, Haihong Zhong, Armelle Logie, Mitchell Revill, Liang Xie, Jingchuan Zhang, De-Hua Yu, Clare Murray, and Paul D. Smith Cancer Res April 15, 2012 72:3224; doi:10.1158/1538-7445.AM2012-3224 .

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5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione

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