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BAY-8002 is an inhibitor of monocarboxylate transporter 1 (MCT1; IC50 = 11.4 nM).1 It inhibits lactate uptake in DLD-1 cells expressing human MCT1 (IC50 = 85 nM) but not Evsa-T cells expressing human MCT4 (IC50 = >50 µM).1 It inhibits the proliferation of 24 cancer cell lines when used at a concentration of 10 µM. BAY-8002 (50 and 100 mg/kg) reduces intratumor lactate levels and tumor area in a Raji mouse xenograft model.
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1. Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-