Chemical Name: 2-[[2-Chloro-5-(phenylsulfonyl)benzoyl]amino]benzoic acid
Biological ActivityBAY 8002 is a 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.
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.
Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-8002 and associated markers of resistance.
Quanz et al.
Mol.Cancer Ther., 2018;17:2285
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