2. Membrane Transporter/Ion Channel
  3. GLUT
  4. WZB117

WZB117 是一种葡萄糖转运蛋白 1 (Glut1) 抑制剂，可下调糖酵解，诱导细胞周期停滞，并在体内外抑制癌细胞生长。

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WZB117 Chemical Structure

WZB117 Chemical Structure

CAS No. : 1223397-11-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥600
In-stock
10 mg ￥910
In-stock
25 mg ￥1650
In-stock
50 mg ￥2450
In-stock
100 mg ￥3430
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

WZB117 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target[1]

GLUT1

 

体外研究
(In Vitro)

Glucose uptake assays show that WZB117 inhibits glucose transport in cancer cells in a dose-dependent manner. The inhibition of glucose transport induced by WZB117 occurres within 1 minute after the assay started, suggesting that the inhibitory activity is likely to be via a direct and fast mechanism. Cell viability assay shows that WZB117 inhibits cancer cell proliferation with an IC50 of approximately 10 μM. The inhibitory activity of WZB117 on cancer cell growth is also confirmed with a clonogenic assay, which also indicates that the inhibition is irreversible in nature. WZB117 treatment results in significantly more cell growth inhibition in lung cancer A549 cells than in nontumorigenic lung NL20 cells. Similar results are also observed in breast cancer MCF7 cells and their nontumorigenic MCF12A cells. When WZB117 is added to cancer cells grown under hypoxic conditions, more cell growth inhibition is observed than under normoxic conditions[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

WZB117 相关抗体:
体内研究
(In Vivo)

The animal study shows that after daily intraperitoneal injection of WZB117 at 10 mg/kg body weight, the sizes of the compound-treated tumors are on average more than 70% smaller than those of the mock (PBS/DMSO)-treated tumors. Notably, 2 of the 10 compound-treated tumors disappear during the treatment and never grow back even at the end of the study. Body weight measurement and analysis reveal that the mice treated with WZB117 lost about 1 to 2 grams of body weight compared with the mock-treated mice with most of the weight loss in the fat tissue. Blood counts and analysis of mice at the end of the study show that lymphocytes and platelets are changed in the compound-treated mice compared with the vehicle-treated mice, but the cell counts remained in the normal ranges. One of the concerns for using glucose transport inhibitors is that the inhibitor might produce hyperglycemia in the treated mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

368.31

Formula

C20H13FO6
CAS 号
性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (678.78 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7151 mL 13.5755 mL 27.1510 mL
5 mM 0.5430 mL 2.7151 mL 5.4302 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用， -20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.79 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.79 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.93%

COA (190 KB) HNMR (201 KB) LCMS (138 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Human non-small cell lung cancer (NSCLC) cell lines H1299 and A549, human breast ductal carcinoma MCF7, as well as human nontumorigenic NL20 lung and MCF12A breast cells are maintained in cell culture media. Cells are treated with WZB117 for 24 or 48 hours. WZB117 (10 μM) is used in the experiments unless otherwise noted. Mock-treated and glucose deprivation samples served as negative and positive controls, respectively. In glucose deprivation, Dulbecco's Modified Eagle's Media (DMEM) with reduced glucose concentration (2 mM or 8% of glucose concentration in the regular cell culture medium) is prepared by mixing glucose-free DMEM with regular DMEM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Male NU/J nude mice of 6 to 8 weeks of age are used. To determine the in vivo anticancer efficacy of WZB117 on human tumor xenograft growth, NSCLC A549 cells in exponential growth phase are harvested, washed, precipitated, and resuspended in PBS. Each mouse is injected subcutaneously with 5×106 cancer cells in the flank. Compound treatment started 3 days after the cancer cells injection and when all tumors become palpable. Tumor cell–injected mice are randomly divided into 2 groups: control group (n=10) treated with PBS/DMSO (1:1, v/v) and WZB117 treatment group (n=10) treated with WZB117 (10 mg/kg body weight) dissolved in PBS/DMSO solution (1:1, v/v). Mice are given intraperitoneal injection with either PBS/DMSO vehicle or WZB117 (10 mg/kg) daily for 10 weeks. Tumor sizes are measured every 7 days with calipers, and tumor volume is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

WZB117 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用， -20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7151 mL 13.5755 mL 27.1510 mL 67.8776 mL
5 mM 0.5430 mL 2.7151 mL 5.4302 mL 13.5755 mL
10 mM 0.2715 mL 1.3576 mL 2.7151 mL 6.7878 mL
15 mM 0.1810 mL 0.9050 mL 1.8101 mL 4.5252 mL
20 mM 0.1358 mL 0.6788 mL 1.3576 mL 3.3939 mL
25 mM 0.1086 mL 0.5430 mL 1.0860 mL 2.7151 mL
30 mM 0.0905 mL 0.4525 mL 0.9050 mL 2.2626 mL
40 mM 0.0679 mL 0.3394 mL 0.6788 mL 1.6969 mL
50 mM 0.0543 mL 0.2715 mL 0.5430 mL 1.3576 mL
60 mM 0.0453 mL 0.2263 mL 0.4525 mL 1.1313 mL
80 mM 0.0339 mL 0.1697 mL 0.3394 mL 0.8485 mL
100 mM 0.0272 mL 0.1358 mL 0.2715 mL 0.6788 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WZB1171223397-11-2WZB 117WZB-117GLUTGlucose transporterInhibitorinhibitorinhibit

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