|3-氟-1,2-亚苯基双(3-羟基苯甲酸酯)|CsnPharm

CAS No.: 1223397-11-2

3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate) Catalog No. CSN19220

Synonyms: Glucose Transporter Inhibitor IV

WZB117 is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 μM.

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400-920-2911

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技术信息

生物活性

描述Glycolysis upregulation can be an important part of understanding cancer and anticancer categories which is primarily related to the upregulated glucose transporter 1 (GLUT1), one of the glucose transporters taking responsibility for basal glucose transport. WZB117 is a representative GLUT1 inhibitor with an IC50 value of 10μM for cancer cell proliferation inhibition. WZB117 could inhibit glucose transport quickly within 1 minute after treatment in a dose-dependent irreversible manner. In A549 cells, MCF7 cells and MCF12A cells, treatment with WZB117 at 30μM showed significant cell growth inhibition, especially under hypoxic condition. Furthermore, injection of 10 mg/kg of this drug in mice tumor models evenly showed >70% smaller than those of the control with a losing about 1 to 2 grams of body weight, which also demonstrated changing of lymphocytes and platelets without generating persistent hyperglycemia. And this effect disappeared 2 hours after injection. WZB117 could also decrease phosphorylated Akt and mTOR within 12 hours accompanied by upregulation of ATP phosphorylation and declination of ATP levels, meaning the loss of its rescue ability. Furthermore, the protein level of GRP78/BiP increased and coincided with glycosylation dysfunction and declination of GLUT1 level. Treatment with WZB117 also resulted in 8% increase in necrosis, 2% apoptosis, 23% cells in G0–G1 phase, 4% cells in G2–M phases and 30% in less S-phase. Injection with WZB117 at 10 mg/kg led to effective inhibition of pRBCs growth in mice. WZB117 at 120μM competitively inhibited GLUTs accompanied by intracellular 95% increasing of reactive oxygen species level.
动物研究
剂量
Mice: 5 mg/kg^[2] (i.p.), 10 mg/kg^[1] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 5 mg/kg^[2] (i.p.), 10 mg/kg^[1] (i.p.)
给药途径	i.p.

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
- 2.7151 mL
- 13.5754 mL
- 27.1509 mL
- 5 mM
- 0.5430 mL
- 2.7151 mL
- 5.4302 mL
- 10 mM
- 0.2715 mL
- 1.3575 mL
- 2.7151 mL

技术信息

CAS号

1223397-11-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H13FO6

运输

蓝冰

分子量

368.31

别名

Glucose Transporter Inhibitor IV

溶解度

DMSO	600.0 mg/mL (1629.1 mM) warming
Water	insoluble

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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3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate) Catalog No. CSN19220

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