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
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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