AR-C155858

Name: AR-C155858
Brand: Tocris Bioscience
SKU: 4960
Rating: 4 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4960

(1)

Citations (70)

COA / SDS

MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells

Key Product Details

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)
Molecular Weight:	461.53

View Full Technical Details for AR-C155858

Technical Data
Citations / Reviews (1)

Biological Activity for AR-C155858

AR-C155858 is an inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (K_i 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 for AR-C155858

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for AR-C155858

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 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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References for AR-C155858

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