AR-C155858

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Cat.No. 4960 - AR-C155858 | C21H27N5O5S | CAS No. 496791-37-8
Description: MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells
Chemical Name: 6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews (1)
Literature

Biological Activity

Inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and <10 nM respectively). Exhibits no activity at MCT4. Blocks proliferation of Raji lymphoma cells in vitro. Inhibits glycolysis and glutathione synthesis in cancer cells.

Licensing Information

Sold for research purposes under agreement from AstraZeneca UK Limited

Technical Data

M. Wt 461.53
Formula C21H27N5O5S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 496791-37-8
PubChem ID 10226546
InChI Key ISIVOJWVBJIOFM-ZDUSSCGKSA-N
Smiles O=C(N4OC[C@@H](O)C4)C1=C(CC3=C(C)NN=C3C)SC(N2CC(C)C)=C1C(N(C)C2=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.15 100

Preparing Stock Solutions

The following data is based on the product molecular weight 461.53. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.17 mL 10.83 mL 21.67 mL
5 mM 0.43 mL 2.17 mL 4.33 mL
10 mM 0.22 mL 1.08 mL 2.17 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Ovens et al (2010) The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem.J. 431 217 PMID: 20695846

Ovens et al (2010) AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem.J. 425 523 PMID: 19929853

Doherty et al (2014) Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis. Cancer Res. 74 908 PMID: 24285728


If you know of a relevant reference for AR-C155858, please let us know.

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Keywords: AR-C155858, supplier, monocarboxylate, transporters, MCT1, MCT2, inhibitors, inhibits, Monocarboxylate, Transporters, Monocarboxylate, Transporters, Tocris Bioscience

2 Citations for AR-C155858

Citations are publications that use Tocris products. Selected citations for AR-C155858 include:

Haas et al (2015) Lactate Regulates Metabolic and Pro-inflammatory Circuits in Control of T Cell Migration and Effector Functions. Nat Commun 13 e1002202 PMID: 26181372

Jamali et al (2015) Hypoxia-induced carbonic anhydrase IX facilitates lactate flux in human breast cancer cells by non-catalytic function. Sci Rep 5 13605 PMID: 26337752


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Reviews for AR-C155858

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Blocking MCT activity in small intestine
By Anonymous on 02/12/2018
Assay Type: Ex Vivo
Species: Rat
Cell Line/Tissue: Wistar

To transiently block uptake capacity of MCT receptors in small intestine of in an ex vivo rodent model

Only partial blockage achieved at selected concentration


Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis