BAY-876

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Chemical Structure| 1799753-84-6 同义名 : -
CAS号 : 1799753-84-6
货号 : A863389
分子式 : C24H16F4N6O2
纯度 : 99%+
分子量 : 496.42
MDL号 : MFCD30377201
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • GLUT1

    GLUT1, IC50:0.002 μM

  • GLUT1

    GLUT1, IC50:0.002 μM
描述 The glucose transporter GLUT1 is overexpressed in various types of human cancers. BAY-876 is a highly selective GLUT1 inhibitor with an IC50 value of 2 nM. The IC50 values of BAY-876 for GLUT2, 3, and 4 are 10.8, 1.67, and 0.29 µM[2]. The treatment with BAY-876 (25 – 75 nM) decreased glycolytic rates in SKOV-3, OVCAR-3, and HEY cells in a dose-dependent manner. BAY-876 at doses of 75 nM reduced basal and CoCl2-stimulated glycolysis in SKOV-3, OVCAR-3, and HEY cells. Incubation of SKOV-3 and OVCAR-3 cells with 75 nM BAY-876 caused a significant decrease in cellular ATP level. BAY-876 also inhibited the mitochondrial activity of viable cells with IC50 values of 60, 188, and 1002 nM for OVCAR-3, SKOV-3, and HEY cells, respectively. In female NSG mice carrying SKOV-3 xenografts, the administration of BAY-876 (1.5 - 4.5 mg/kg/day) for 4 weeks does-dependently inhibited tumor growth as compared to the group received no BAY-876 treatment[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.07mL

2.01mL

1.01mL

20.14mL

4.03mL

2.01mL
参考文献

[1]Siebeneicher H, Cleve A, et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Oct 19;11(20):2261-2271.

[2]Siebeneicher H, Cleve A, Rehwinkel H, et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016;11(20):2261-2271. doi:10.1002/cmdc.201600276

[3]Ma Y, Wang W, Idowu MO, et al. Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876. Cancers (Basel). 2018;11(1):33. Published 2018 Dec 31. doi:10.3390/cancers11010033