Molecular Formula | C20H14ClNO5S |
Molar Mass | 415.85 |
Solubility | DMSO : 125 mg/mL (300.59 mM; Need ultrasonic);H2O : < 0.1 mg/mL (insoluble) |
Storage Condition | Sealed in dry,Room Temperature |
In vitro study | In DLD-1 cells expressing MCT1, BAY-8002 can inhibit the fluorescence changes of intracellular SNARF-5, and the IC50 is 85 (6) nmol/L. In EVSA-T cells, the selectivity for MCTL is high, whereas the IC50 for MCT4 is greater than 50 μm. BAY-8002 is a dual inhibitor of MCT1 and mct2. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.405 ml | 12.024 ml | 24.047 ml |
5 mM | 0.481 ml | 2.405 ml | 4.809 ml |
10 mM | 0.24 ml | 1.202 ml | 2.405 ml |
5 mM | 0.048 ml | 0.24 ml | 0.481 ml |
biological activity | BAY-8002 is a novel MCT1 inhibitor that can effectively inhibit the bidirectional transport of lactate. BAY-8002 can significantly increase the level of lactic acid in the tumor and transiently regulate the content of pyruvate. |
Target | Value |
Animal Model: | Female NOD SCID mice bearing Raji cells (7-10 weeks old) |
Dosage: | 80 and 160 mg/kg |
Administration: | P.O. twice daily for more than 26 days |
Result: | Inhibited tumor growth with no obvious body weight loss, but showed no effect on tumor regression. |