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CAS No.: 1799753-84-6

BAY-876 Catalog No. CSN18813

Synonyms: BAY-876

BAY-876 is a selective inhibitor of GLUT1 with IC50 of 0.002 μM with good metabolic stability.

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技术信息

生物活性

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0144 mL
- 10.0722 mL
- 20.1444 mL
- 5 mM
- 0.4029 mL
- 2.0144 mL
- 4.0289 mL
- 10 mM
- 0.2014 mL
- 1.0072 mL
- 2.0144 mL

技术信息

CAS号

1799753-84-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H16F4N6O2

运输

蓝冰

分子量

496.42

别名

BAY-876

溶解度

DMSO	97.0 mg/mL (195.4 mM) warming
Water	Insoluble
Ethanol	3.0 mg/mL (6.0 mM) warming

动物实验配方

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