S80476 |
BAY-876 |
| 源叶(MedMol) | 98% |
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- 产品描述： BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4[1]. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth
- 靶点： GLUT1:2 nM (IC50);GLUT2:10.08 μM (IC50);GLUT3:1.67 μM (IC50);GLUT4;0.29 μM (IC50)
- 体外研究： BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells. Cell Proliferation Assay Cell Line: SKOV-3 and OVCAR-3 cells Concentration: 25, 50, 75 nM Incubation Time: 24 and 72 hours Result: Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.
- 体内研究： BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice. Animal Model: Female NOD-scid IL2rgnull (NSG) mice carrying SKOV-3 subcutaneous (s.c.) xenografts Dosage: 1.5, 3, 4.5 mg/kg Administration: Oral administration; daily; for 28 days Result: Caused a clear dose-dependent inhibition of tumorigenicity.
- 参考文献：
1. Siebeneicher H et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Aug 23. 2. Ma Y, et al. Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876. Cancers (Basel). 2018 Dec 31;11(1).
- 溶解性： Soluble in DMSO、Methanol
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.014 ml 10.072 ml 20.144 ml 5 mM 0.403 ml 2.014 ml 4.029 ml 10 mM 0.201 ml 1.007 ml 2.014 ml 50 mM 0.04 ml 0.201 ml 0.403 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
