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AB286958

AZD-3965

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(1 Publication)

MW 515.5 Da, Purity >98%. A potent and selective monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM; it is 6-fold selective over MCT2 and does not inhibit MCT4 even at 10 μM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.

View Alternative Names

FLJ36745, HHF7, MCT, MCT 1, MGC44475, MOT1_HUMAN, Monocarboxylate transporter, Monocarboxylate transporter 1, Monocarboxylate transporter isoform 1, Monocarboxylic acid transporter 1, SLC16A1 protein, Slc16a1, Solute carrier family 16 (monocarboxylic acid transporters) member 1, Solute carrier family 16 member 1, Solute carrier family 16 member 1 (monocarboxylic acid transporter 1)

Key facts

CAS number

1448671-31-5

Purity

>98%

Form

Solid

form

Molecular weight

515.5 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>4</sub>F<sub>3</sub>N<sub>5</sub>O<sub>5</sub>S

PubChem

10369242

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 100 mM

Biochemical name

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

Biological description

A potent and selective monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM; it is 6-fold selective over MCT2 and does not inhibit MCT4 even at 10 μM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.

Canonical 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

Isomeric 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)N4C[C@](CO4)(C)O

InChi

InChI=1S/C21H24F3N5O5S/c1-9(2)29-18-14(16(30)27(5)19(29)32)13(17(31)28-7-20(4,33)8-34-28)12(35-18)6-11-10(3)25-26-15(11)21(22,23)24/h9,33H,6-8H2,1-5H3,(H,25,26)/t20-/m0/s1

InChiKey

PRNXOFBDXNTIFG-FQEVSTJZSA-N

IUPAC Name

5-[(4S)-4-hydroxy-4-methyl-1,2-oxazolidine-2-carbonyl]-3-methyl-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-1-propan-2-ylthieno[2,3-d]pyrimidine-2,4-dione

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2227 AZD-3965. B2227-1 is the same size as the 1 mg size of ab286958.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store in the dark|Store under desiccating conditions|This product is air and light sensitive and impurities can occur as a result of air oxidation or due to metabolism by microbes
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

MCT1 also known as Monocarboxylate Transporter 1 or SLC16A1 is a protein that facilitates the transport of monocarboxylates such as lactate and pyruvate across cell membranes. The approximate molecular weight of MCT1 is 51 kDa. This transporter expresses in many tissues including muscle brain liver and kidney. Its widespread presence indicates a significant role in cellular metabolism and energy balance across different biological systems.
Biological function summary

MCT1 acts as an important transport mechanism for lactate and pyruvate driving the cellular uptake and release processes of these molecules. It partners with CD147 also known as Basigin to form a functional heteromeric complex. This binding allows the correct localization and stabilization of MCT1 in the plasma membrane ensuring effective transport activity. The presence of MCT1 in metabolically active tissues highlights its role in maintaining homeostasis in energy-rich environments.

Pathways

MCT1 plays a significant role in the glycolysis and gluconeogenesis pathways by mediating lactate transport which connects anaerobic and aerobic metabolic processes. Through these pathways MCT1 associates with key metabolic enzymes like lactate dehydrogenase (LDH) that regulate the conversion between lactate and pyruvate. This association provides a link between lactate production and consumption thereby controlling pH levels and preventing the buildup of metabolic intermediates that can disrupt cellular functions.

MCT1 is implicated in cancer and metabolic acidosis. In cancer elevated expression of MCT1 supports the Warburg effect a phenomenon where cancer cells rely on aerobic glycolysis leading to increased lactate production. MCT1 works alongside proteins such as CD147 influencing tumor growth and metastasis by promoting lactate export. In metabolic acidosis impaired MCT1 function can disrupt lactate clearance affecting tissue pH balance and contributes to conditions like lactic acidosis. Understanding MCT1's role in these diseases highlights the importance of targeting its function for therapeutic purposes.
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Product protocols

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Publications (1)

Recent publications for all applications. Explore the full list and refine your search

Molecular cancer therapeutics 13:2805-16 PubMed25281618

2014

Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport.

Applications

Unspecified application

Species

Unspecified reactive species

Becky M Bola,Amy L Chadwick,Filippos Michopoulos,Kathryn G Blount,Brian A Telfer,Kaye J Williams,Paul D Smith,Susan E Critchlow,Ian J Stratford
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