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Chemical Structure : BAY-8002
Catalog No.: PC-35589Not For Human Use, Lab Use Only.
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.
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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.
| M.Wt | 415.844 | |
| Formula | C20H14ClNO5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Quanz M, et al. Mol Cancer Ther. 2018 Aug 16. pii: molcanther.1253.2017.
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