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