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
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500 mg   询价  

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WZB117 相关抗体

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GLUT1 GLUT2 GLUT3 GLUT4

  • 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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 10 μM
Compound: 46830365
Inhibition of the Glucose Transporter (GLUT1, SLC2A1) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A1 WT-OE cells
Inhibition of the Glucose Transporter (GLUT1, SLC2A1) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A1 WT-OE cells
10.5281/zenodo.7360676
HEK293 IC50
> 10 μM
Compound: 46830365
Inhibition of the Glucose Transporter (GLUT2, SLC2A2) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A2 WT-OE cells
Inhibition of the Glucose Transporter (GLUT2, SLC2A2) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A2 WT-OE cells
10.5281/zenodo.7360664
HEK293 IC50
> 10 μM
Compound: 46830365
Inhibition of the Glucose Transporter (GLUT3, SLC2A3) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A3 WT-OE cells
Inhibition of the Glucose Transporter (GLUT3, SLC2A3) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A3 WT-OE cells
10.5281/zenodo.7360656
HEK293 IC50
2.5 μM
Compound: 46830365
Inhibition of the Glucose Transporter (GLUT4, SLC2A4) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A4 WT-OE cells
Inhibition of the Glucose Transporter (GLUT4, SLC2A4) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A4 WT-OE cells
10.5281/zenodo.7360638
NCI-H1299 IC50
20.4 μM
Compound: WZB117
Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay
[PMID: 24200808]
体外研究
(In Vitro)

WZB117 抑制癌细胞的葡萄糖转运呈剂量依赖性；该作用在实验开始后 1 分钟内发生，提示其通过直接快速机制发挥作用。细胞活力检测显示，WZB117 抑制癌细胞增殖的 IC50 约为 10 μM。克隆形成实验表明其对癌细胞的抑制作用不可逆。WZB117 对肺癌 A549 细胞的抑制作用显著强于非肿瘤性 NL20 细胞，在乳腺癌 MCF7 细胞和非肿瘤性 MCF12A 细胞中观察到类似结果；在缺氧条件下，WZB117 对癌细胞的生长抑制作用更明显[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)

动物研究显示，每日腹膜内注射 10 mg/kg 体重的 WZB117 后，化合物治疗的肿瘤大小平均比模拟(PBS/DMSO)治疗的肿瘤小 70% 以上。值得注意的是，10 个化合物治疗的肿瘤中有 2 个在治疗期间消失，即使在研究结束时也从未再生长。体重测量和分析显示，与模拟治疗的小鼠相比，用 WZB117 治疗的小鼠体重减轻了约 1 至 2 克，大部分体重减轻在脂肪组织中。研究结束时对小鼠的血细胞计数和分析表明，与载体治疗的小鼠相比，化合物治疗的小鼠的淋巴细胞和血小板发生了变化，但细胞计数仍在正常范围内。使用葡萄糖转运抑制剂的一个担忧是该抑制剂可能会在治疗的小鼠中产生高血糖症[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。

    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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