AR-C155858
Tocris Bioscience, part of Bio-Techne | Catalog # 4960
MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells
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 LimitedProduct Specifications
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.
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Ovens 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. 2010 PMID: 19929853
- Doherty Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis. Cancer Res. 2014 PMID: 24285728
- Ovens The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem.J. 2010 PMID: 20695846
Product Specific Notices for AR-C155858
For research use only
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