| 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);transporter |
| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京