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Potent dual MCT1/2 inhibitor (IC50 values are 3, 8, and 12 nM at rat (C6), human (DLD-1) and mouse (4T1) MCT1 respectively; IC50 values of human MCT1, MCT2, and MCT4 isoforms recombinantly expressed in X. laevis oocytes are 1, 5 and >500 nM, respectively); suppresses bidirectional lactate transport. Inhibits cellular SNARF-5 fluorescence change (IC50 = 85 nM) in MCT1-expressing DLD-1 cells. Arrests growth and increases intratumor lactate levels of Raji tumor xenografts in mice. Orally bioavailable.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 415.85. 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||2.4 mL||12.02 mL||24.05 mL|
|5 mM||0.48 mL||2.4 mL||4.81 mL|
|10 mM||0.24 mL||1.2 mL||2.4 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the biological activity of the product.
Quanz et al (2018) Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-8002 and associated markers of resistance. Mol.Cancer Ther. 17 2285 PMID: 30115664
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Keywords: BAY 8002, BAY 8002 supplier, BAY8002, potent, dual, MCT1/2, inhibitors, inhibits, MCT1, MCT2, orally, bioavailable, lactate, Monocarboxylate, Transporters, 6817, Tocris Bioscience
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