AR-C155858

Tocris Bioscience | Catalog # 4960

MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells
Tocris Bioscience
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Key Product Details

Description

MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells

Product Description

AR-C155858 is an 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

Product Specifications for AR-C155858

Molecular Weight

461.53

Formula

C21H27N5O5S

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

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Solubility

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

Preparing Stock Solutions for AR-C155858

The following data is based on the product molecular weight 461.53.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 80 publications citing the usage of this product.

Product Documents for AR-C155858

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for AR-C155858

For research use only

Customer Reviews for AR-C155858 (2)

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Showing  1 - 2 of 2 reviews Showing All
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  • Oocyte inhibition
    Name: Murali K Yanda
    Species: Mouse
    Assay Type: In Vitro
    Cell Line/Tissue: Oocytes
    Verified Customer | Posted 11/13/2023
    Inhibition of L-lactate transport activity at pH 6 by increasing concentrations of AR-C155858 was determined using 0.5 mM L-[14C]lactate (pH 6).
    AR-C155858 4960
  • Blocking MCT activity in small intestine
    Name: Tauseef Ahmad
    Assay Type: Ex Vivo
    Cell Line/Tissue: Wistar
    Verified Customer | Posted 02/12/2018
    Only partial blockage achieved at selected concentration
    To transiently block uptake capacity of MCT receptors in small intestine of in an ex vivo rodent model
    AR-C155858 4960

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