| References: |
BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM), inhibits cellular lactate uptake in DLD-1 cells with IC50 of 8 nM; displays no significant activity against in MCT4 expressing cells; inhibits cellular SNARF-5 fluorescence change with an IC50 of 85 nM in MCT1-expressing DLD-1 cells and displays excellent selectivity against MCT4 (IC50 >50 uM in EVSA-T cells); inhibits lactate uptake in MCT2-expressing oocytes, with ~5-fold lower potency compared to the MCT1 isoform; significantly increases intratumor lactate levels and transiently modulates pyruvate levels, inhibits Raji (IC50=0.67 uM) but not WSU-DLCL2 tumor growth. |
