S88706 |
BAY-8002 |
源叶(MedMol) | 98% |
- 产品描述: BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity
- 靶点: IC50: 85 nM (MCT1, in DLD-1 cells);Monocarboxylatetransporter
- 体外研究:
BAY-8002 is an inhibitor of MCT1, with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4 (IC50 >50 µM in EVSA-T cells)
- 体内研究:
BAY-8002 (80 and 160 mg/kg, p.o., twice daily, for more than 26 days) significantly inhibits tumor growth in Raji tumor-bearing mice. 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.
- 参考文献:
1. Quanz M, et al. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Nov;17(11):2285-2296.
- 溶解性: Soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
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 50 mM 0.048 ml 0.24 ml 0.481 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)