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

WZB117 是一種葡萄糖轉(zhuǎn)運(yùn)蛋白 1 (Glut1) 抑制劑，可下調(diào)糖酵解，誘導(dǎo)細(xì)胞周期停滯，并在體內(nèi)外抑制癌細(xì)胞生長。

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WZB117 Chemical Structure

WZB117 Chemical Structure

CAS No. : 1223397-11-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥486
In-stock
1 mg ￥273
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 ￥5163
In-stock
500 mg   詢價(jià)  
1 g   詢價(jià)  

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查看 GLUT 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(In Vitro)

WZB117 抑制癌細(xì)胞的葡萄糖轉(zhuǎn)運(yùn)呈劑量依賴性；該作用在實(shí)驗(yàn)開始后 1 分鐘內(nèi)發(fā)生，提示其通過直接快速機(jī)制發(fā)揮作用。細(xì)胞活力檢測顯示，WZB117 抑制癌細(xì)胞增殖的 IC50 約為 10 μM?？寺⌒纬蓪?shí)驗(yàn)表明其對癌細(xì)胞的抑制作用不可逆。WZB117 對肺癌 A549 細(xì)胞的抑制作用顯著強(qiáng)于非腫瘤性 NL20 細(xì)胞，在乳腺癌 MCF7 細(xì)胞和非腫瘤性 MCF12A 細(xì)胞中觀察到類似結(jié)果；在缺氧條件下，WZB117 對癌細(xì)胞的生長抑制作用更明顯[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

動(dòng)物研究顯示，每日腹膜內(nèi)注射 10 mg/kg 體重的 WZB117 后，化合物治療的腫瘤大小平均比模擬(PBS/DMSO)治療的腫瘤小 70% 以上。值得注意的是，10 個(gè)化合物治療的腫瘤中有 2 個(gè)在治療期間消失，即使在研究結(jié)束時(shí)也從未再生長。體重測量和分析顯示，與模擬治療的小鼠相比，用 WZB117 治療的小鼠體重減輕了約 1 至 2 克，大部分體重減輕在脂肪組織中。研究結(jié)束時(shí)對小鼠的血細(xì)胞計(jì)數(shù)和分析表明，與載體治療的小鼠相比，化合物治療的小鼠的淋巴細(xì)胞和血小板發(fā)生了變化，但細(xì)胞計(jì)數(shù)仍在正常范圍內(nèi)。使用葡萄糖轉(zhuǎn)運(yùn)抑制劑的一個(gè)擔(dān)憂是該抑制劑可能會(huì)在治療的小鼠中產(chǎn)生高血糖癥[1]。

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

368.31

Formula

C20H13FO6
CAS 號
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 250 mg/mL (678.78 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.93%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
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產(chǎn)品名稱：
WZB117
目錄號：
HY-19331
需求量：