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Description: BAY-8002 is a novel, potent, selective, and orally bioactive inhibitor of monocarboxylate transporter 1 (MCT1) with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, it displays excellent selectivity against MCT4. Anti-tumor activity. The lactate transporter SLC16A1/monocarboxylate transporter 1 (MCT1) plays a central role in tumor cell energy homeostasis. BAY-8002 potently suppress bidirectional lactate transport. BAY-8002 significantly increased intratumor lactate levels and transiently modulated pyruvate levels.
References: Mol Cancer Ther. 2018 Nov; 17(11):2285-2296.
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