BAY-876
目录号: PL01015 纯度: ≥98%
CAS No. :1799753-84-6
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中文名称
BAY-876
中文别名
BAY-876
英文名称
BAY-876
英文别名
BAY-876;BAY876;N4-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoro-2,4-quinolinedicarboxamide;BAY 876;N4-(1-(4-Cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-7-fluoroquinoline-2,4-dicarboxamide;BCP25065;s8452;SB19770;N4-{1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl}-7-fluoroquinoline-2,4-dicarboxamide;2,4-Quinoline;4-N-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicar
Cas No.
1799753-84-6
分子式
C24H16F4N6O2
分子量
496.42
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
BAY-876 是一种具有口服活性的,选择性的葡萄糖转运蛋白 1 (GLUT1) 抑制剂,IC50 为 2 nM。BAY-876 对 GLUT1 的选择性是 GLUT2,GLUT3 和 GLUT4 的 130 倍以上。BAY-876 还是一种糖酵解代谢和卵巢癌生长的有效阻滞剂。
生物活性
BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC 50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
性状
Solid
IC50 & Target[1][2]
GLUT1 2 nM (IC50) GLUT2 10.08 μM (IC5
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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).
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (201.44 mM)Methanol : 1 mg/mL (2.01 mM; ultrasonic and warming and heat to 60°C)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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