BAY-8002 is an orally available, potent and selective inhibitor of lactate transporter MCT1 (monocarboxylate transporter 1; SLC16A1) that potently inhibits bidirectional lactate transport. BAY-8002 exhibits antiproliferative activity in numerous cancer cell lines. BAY-8002 induces accumulation of lactate and significantly inhibits tumor growth in mice model. It does not cause tumor regression.
orally available, potent and selective inhibitor of lactate transporter MCT1
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11 - Combustible Solids
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WGK 3
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Molecular cancer therapeutics, 17(11), 2285-2296 (2018-08-18)
The lactate transporter SLC16A1/monocarboxylate transporter 1 (MCT1) plays a central role in tumor cell energy homeostasis. In a cell-based screen, we identified a novel class of MCT1 inhibitors, including BAY-8002, which potently suppress bidirectional lactate transport. We investigated the antiproliferative
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