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WZB117 {[allProObj[0].p_purity_real_show]}

货号:A135447

WZB117是葡萄糖转运蛋白 1(GLUT1)的抑制剂,能够抑制肺癌 A549 细胞和乳腺癌 MCF7 细胞的增殖,IC50 约为 10 μM。

WZB117 化学结构 CAS号:1223397-11-2
WZB117 化学结构
CAS号:1223397-11-2
WZB117 3D分子结构
CAS号:1223397-11-2
WZB117 化学结构 CAS号:1223397-11-2
WZB117 3D分子结构 CAS号:1223397-11-2
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WZB117 纯度/质量文件 产品仅供科研

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产品名称 GLUT1 其他靶点 纯度
STF-31 99%+
BAY-876 +++

GLUT1, IC50: 0.002 μM

99%+
WZB117 ++

GLUT1, IC50: 10μM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

WZB117 生物活性

靶点
  • GLUT1

    GLUT1, IC50:10μM

描述 WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo[1]. WZB117 impedes glucose transport into cancer cells in a dose-responsive manner as shown by glucose uptake assays. This blockage occurs rapidly, within 1 minute of assay initiation, indicating a direct and swift mode of action. Cell viability assays demonstrate WZB117's capacity to inhibit cancer cell proliferation with an IC50 value around 10 μM. Clonogenic assays further validate WZB117's suppressive effect on cancer cell growth, suggesting this effect is irreversible. WZB117 treatment leads to more pronounced growth inhibition in lung cancer A549 cells compared to non-tumorigenic NL20 lung cells, with similar trends observed between breast cancer MCF7 cells and non-tumorigenic MCF12A cells. Under hypoxic conditions, cancer cells exhibit increased sensitivity to WZB117 compared to normoxic conditions[1].
体内研究

In animal studies, daily intraperitoneal injections of WZB117 at 10 mg/kg body weight significantly reduce tumor sizes by more than 70% compared to tumors in mock-treated mice. Body weight measurements indicate that WZB117-treated mice experience a weight loss of about 1 to 2 grams, primarily from fat tissue, compared to mock-treated mice[1].

体外研究

WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo[1].

WZB117 impedes glucose transport into cancer cells in a dose-responsive manner as shown by glucose uptake assays. This blockage occurs rapidly, within 1 minute of assay initiation, indicating a direct and swift mode of action. Cell viability assays demonstrate WZB117's capacity to inhibit cancer cell proliferation with an IC50 value around 10 μM. Clonogenic assays further validate WZB117's suppressive effect on cancer cell growth, suggesting this effect is irreversible. WZB117 treatment leads to more pronounced growth inhibition in lung cancer A549 cells compared to non-tumorigenic NL20 lung cells, with similar trends observed between breast cancer MCF7 cells and non-tumorigenic MCF12A cells. Under hypoxic conditions, cancer cells exhibit increased sensitivity to WZB117 compared to normoxic conditions[1].

WZB117 动物研究

Dose Mice: 5 mg/kg[2] (i.p.), 10 mg/kg[1] (i.p.)
Administration i.p.

WZB117 参考文献

[1]Liu Y, et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol Cancer Ther. 2012 Aug;11(8):1672-82.

WZB117 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.58mL

2.72mL

1.36mL

27.15mL

5.43mL

2.72mL

WZB117 技术信息

CAS号1223397-11-2
分子式C20H13FO6
分子量 368.312
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

DMSO: 145 mg/mL(393.69 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

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