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  1. Anti-infection Apoptosis Cell Cycle/DNA Damage Cytoskeleton
  2. Parasite Apoptosis Microtubule/Tubulin
  3. Mebendazole

甲苯達(dá)唑是一種高效、廣譜的抗線(xiàn)蟲(chóng)藥。甲苯達(dá)唑?qū)Χ嘈涡匀橄倌讣?xì)胞瘤 (GBM) 也有抑制作用,抑制 Hedgehog 通路和微管蛋白 (tubulin) 聚合。甲苯達(dá)唑具有口服活性,可透過(guò)血腦屏障。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Mebendazole Chemical Structure

Mebendazole Chemical Structure

CAS No. : 31431-39-7

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10 mM * 1 mL in DMSO ¥500
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500 mg ¥400
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1 g ¥500
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Customer Review

Other Forms of Mebendazole:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration[1][2][3].

IC50 & Target

Tublin polymerization[1]; Hedgehog[2]; Parasite[3]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 EC50
0.9 μM
Compound: MBZ
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29288939]
A549/TR EC50
1.7 μM
Compound: MBZ
Cytotoxicity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29288939]
Calu-1 EC50
1.1 μM
Compound: MBZ
Cytotoxicity against human Calu1 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human Calu1 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29288939]
HepG2 2.2.15 IC50
> 1000 μM
Compound: 5a
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBsAg secretion after 9 days by ELISA
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBsAg secretion after 9 days by ELISA
[PMID: 25650312]
HepG2 2.2.15 IC50
> 1000 μM
Compound: 5a
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as HBeAg secretion after 9 days by ELISA
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as HBeAg secretion after 9 days by ELISA
[PMID: 25650312]
HepG2 2.2.15 CC50
> 1000 μM
Compound: 5a
Cytotoxicity against human HepG2.2.15 cells assessed as cell death after 9 days by MTS assay
Cytotoxicity against human HepG2.2.15 cells assessed as cell death after 9 days by MTS assay
[PMID: 25650312]
HL-60 EC50
> 30 μM
Compound: 1, mebendazole
Cytotoxicity against human HL60 cells after 48 to 72 hrs by Alamar blue assay
Cytotoxicity against human HL60 cells after 48 to 72 hrs by Alamar blue assay
[PMID: 22795629]
HUVEC IC50
8.8 μM
Compound: Mebendazole
Inhibition of VEGFR2-mediated angiogenesis in human HUVEC cells after 24 hrs by inverted photomicroscopic analysis
Inhibition of VEGFR2-mediated angiogenesis in human HUVEC cells after 24 hrs by inverted photomicroscopic analysis
[PMID: 22780961]
NCI-H157 EC50
3.5 μM
Compound: MBZ
Cytotoxicity against human NCI-H157 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human NCI-H157 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29288939]
PC-3 EC50
1.1 μM
Compound: MBZ
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29288939]
PC-3M EC50
1.21 μM
Compound: MBZ
Cytotoxicity against human PC3M cells assessed as reduction in cell viability after 48 hrs by cyquant reagent based fluorescence spectrometric assay
Cytotoxicity against human PC3M cells assessed as reduction in cell viability after 48 hrs by cyquant reagent based fluorescence spectrometric assay
[PMID: 29288939]
SK-OV-3 EC50
0.5 μM
Compound: MBZ
Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29288939]
體外研究
(In Vitro)

Mebendazole (1 nM-0.1 mM;72 h) 抑制 GL261 小鼠神經(jīng)膠質(zhì)瘤細(xì)胞,IC50 值為 0.24 μM[1]
Mebendazole (0.1 μM 和 1 μM;24 h) 破壞 060919 多形性膠質(zhì)母細(xì)胞瘤 (GBM) 細(xì)胞中的微管聚合和微管結(jié)構(gòu)[1]。
Mebendazole (10 nM-10 μM;48 h) 通過(guò)降低腫瘤組織中的 Gli1 轉(zhuǎn)錄本和蛋白表達(dá),抑制 Hh 信號(hào)并降低下游 Hh 通路效應(yīng)子的表達(dá)。 Mebendazole 抑制 Gli1 表達(dá),IC50 值為 516 nM[2]
Mebendazole (10 nM-10 μM;48 h) 阻止初級(jí)纖毛的形成,并降低具有組成型 Hh 激活的人髓母細(xì)胞瘤細(xì)胞的增殖和存活[2]。
Mebendazole 和 Vismodegib 的組合實(shí)現(xiàn)了對(duì)典型 Hh 信號(hào)的附加抑制[2]
Mebendazole 曾在許多臨床環(huán)境中有效治療中樞神經(jīng)系統(tǒng)包蟲(chóng)病,表明其具有顯著的中樞神經(jīng)系統(tǒng)滲透特性[3]

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

Immunofluorescence[1]

Cell Line: Glioblastoma multiforme (GBM) 060919 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Disrupted microtubule structure.

Immunofluorescence[2]

Cell Line: DAOY and hTERT-RPE1 cells
Concentration: 0, 0.1, 0.5, 0.75, and 1 μM
Incubation Time: 12 hours
Result: Decreased GLI1 protein level and increased cleavage of caspase-3 protein level.
體內(nèi)研究
(In Vivo)

Mebendazole (50 mg/kg; p.o.; once daily for first 20 d and 5 d per week with 2 d off; 45 d) 在同系 GL261 小鼠模型和 060919 人多形性膠質(zhì)母細(xì)胞瘤 (GBM) 異種移植小鼠模型中抑制顱內(nèi)腫瘤生長(zhǎng)[1]。

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

Animal Model: C57BL/6 mice (5-6 weeks old) implanted with GL261 glioma cells and 060919 human glioblastoma multiforme (GBM)[1]
Dosage: 50 mg/kg; delivered with 50% (v/v) sesame oil and PBS[2]
Administration: Oral gavage; beginning 5 days after tumor implantation at a daily dose of 50 mg/kg for the first 20 days of treatment then changed to 50 mg/kg for 5 days, with 2 days off, each week.
Result: Increased the mean survival to 49 days compared with the 30 days of control in syngeneic GL261 mouse model.
Increased the mean survival to 65 days compared with the 48 days of control in 060919 human glioblastoma multiforme (GBM) xenograft mouse model.
Clinical Trial
分子量

295.29

Formula

C16H13N3O3

CAS 號(hào)
性狀

固體

顏色

Off-white to light yellow

中文名稱(chēng)

甲苯咪唑;甲苯達(dá)唑;甲苯噠唑

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 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 4.17 mg/mL (14.12 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.3865 mL 16.9325 mL 33.8650 mL
5 mM 0.6773 mL 3.3865 mL 6.7730 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(qǐng)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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?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(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.42 mg/mL (1.42 mM); 澄清溶液

    此方案可獲得 ≥ 0.42 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 4.2 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(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.42 mg/mL (1.42 mM); 澄清溶液

    此方案可獲得 ≥ 0.42 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 4.2 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。

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑: 50% PEG300    50% Saline

    Solubility: 5 mg/mL (16.93 mM); 懸濁液; 超聲助溶

  • 方案 二

    請(qǐng)依序添加每種溶劑: 15% Cremophor EL    85% Saline

    Solubility: 25 mg/mL (84.66 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)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

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)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(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
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(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)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(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)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: 99.88%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(qǐng)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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?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 3.3865 mL 16.9325 mL 33.8650 mL 84.6625 mL
5 mM 0.6773 mL 3.3865 mL 6.7730 mL 16.9325 mL
10 mM 0.3387 mL 1.6933 mL 3.3865 mL 8.4663 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.

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產(chǎn)品名稱(chēng):
Mebendazole
目錄號(hào):
HY-17595
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