S80476 |
BAY-876 |
源葉(MedMol) | 98% |
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- 產(chǎn)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
- 靶點: GLUT1:2 nM (IC50);GLUT2:10.08 μM (IC50);GLUT3:1.67 μM (IC50);GLUT4;0.29 μM (IC50);transporter
- 體外研究:
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.
- 體內(nèi)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.
- 參考文獻:
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
- 保存條件: -20℃
- 配置溶液濃度參考:
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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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)