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  2. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related Apoptosis
  3. Microtubule/Tubulin ADC Cytotoxin Apoptosis
  4. Monomethyl auristatin E

Monomethyl auristatin E  (Synonyms: MMAE; SGD-1010; Vedotin)

目錄號(hào): HY-15162 純度: 99.97%
COA 產(chǎn)品使用指南 技術(shù)支持

Monomethyl auristatin E (MMAE; SGD-1010) 是海兔毒素 10 的合成衍生物，通過(guò)抑制微管蛋白聚合而起到有效的有絲分裂抑制作用。 MMAE 廣泛用作細(xì)胞毒性成分制作抗體偶聯(lián)活性分子 (ADCs) 用于癌癥的研究。

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)

Monomethyl auristatin E Chemical Structure

Monomethyl auristatin E Chemical Structure

CAS No. : 474645-27-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
5 mg ￥250
In-stock
10 mg ￥400
In-stock
50 mg ￥690
In-stock
100 mg ￥950
In-stock
250 mg ￥1450
In-stock
500 mg ￥2500
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

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Customer Review

Other Forms of Monomethyl auristatin E:

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

Proliferation Assay

    Monomethyl auristatin E purchased from MCE. Usage Cited in: Sci Rep. 2016 Apr 21;6:24954.  [Abstract]

    LC-MS/MS analysis quantified the MMAE concentration in the tumors 3, 24, and 72?h after the administration of MMAE alone. The contents of MMAE in the tumor tissues 3, 24, and 72?h after administration are 1155?±?609, 736?±?319, and 413?±?88?fmol/g (mean?±?SD, N?=?5 for each group), respectively.

    • 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

    Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

    IC50 & Target

    Auristatin

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 EC50
    0.0005 μM
    Compound: Monomethyl auristatin E
    Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
    		[PMID: 28972755]
    A549 IC50
    0.59 nM
    Compound: MMAE
    Antiproliferative activity against human A549 cells after 4 days by XTT assay
    Antiproliferative activity against human A549 cells after 4 days by XTT assay
    		[PMID: 23845743]
    A549 IC50
    1.3 nM
    Compound: 2; MMAE
    Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay
    Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay
    		[PMID: 29454703]
    BT-474 GI50
    0.22 nM
    Compound: 4, MMAE
    Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay
    Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay
    		[PMID: 25431858]
    BXPC-3 GI50
    > 1.39 nM
    Compound: 2b
    Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay
    		[PMID: 28211277]
    BXPC-3 GI50
    > 1.39 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
    Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
    		[PMID: 28926240]
    BXPC-3 GI50
    > 1.39 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
    Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
    		[PMID: 28895394]
    CWR22R CC50
    1.44 nM
    Compound: MMAE
    Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay
    Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay
    		[PMID: 34797052]
    DU-145 GI50
    0.418 nM
    Compound: 2b
    Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay
    		[PMID: 28211277]
    DU-145 GI50
    0.418 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human DU145 cells after 48 hrs by SRB assay
    Growth inhibition of human DU145 cells after 48 hrs by SRB assay
    		[PMID: 28926240]
    DU-145 GI50
    0.418 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human DU145 cells after 48 hrs by SRB assay
    Growth inhibition of human DU145 cells after 48 hrs by SRB assay
    		[PMID: 28895394]
    DU-145 IC50
    0.55 nM
    Compound: MMAE
    Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay
    Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay
    		[PMID: 36327103]
    DU-145 IC50
    0.62 nM
    Compound: MMAE
    Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay
    Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay
    		[PMID: 36327103]
    HeLa IC50
    1 nM
    Compound: MMAE
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay
    		[PMID: 36327103]
    HeLa IC50
    1.1 nM
    Compound: MMAE
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay
    		[PMID: 36327103]
    HGC-27 IC50
    7.18 nM
    Compound: MMAE
    Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay
    Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay
    		[PMID: 35932567]
    KB IC50
    0.19 nM
    Compound: MMAE
    Antiproliferative activity against human KB cells after 4 days by XTT assay
    Antiproliferative activity against human KB cells after 4 days by XTT assay
    		[PMID: 23845743]
    KM-20L2 GI50
    0.599 nM
    Compound: 2b
    Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay
    		[PMID: 28211277]
    KM-20L2 GI50
    0.599 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
    Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
    		[PMID: 28926240]
    KM-20L2 GI50
    0.599 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
    Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
    		[PMID: 28895394]
    L1210 IC50
    2.1 nM
    Compound: 2; MMAE
    Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay
    Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay
    		[PMID: 29454703]
    LNCaP IC50
    0.71 nM
    Compound: MMAE
    Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay
    Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay
    		[PMID: 36327103]
    LNCaP IC50
    0.79 nM
    Compound: MMAE
    Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay
    Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay
    		[PMID: 36327103]
    MCF7 GI50
    0.404 nM
    Compound: 2b
    Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay
    		[PMID: 28211277]
    MCF7 GI50
    0.404 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
    Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
    		[PMID: 28926240]
    MCF7 GI50
    0.404 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
    Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
    		[PMID: 28895394]
    MDA-MB-231 IC50
    0.25 nM
    Compound: MMAE
    Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay
    		[PMID: 23845743]
    MDA-MB-361 GI50
    0.49 nM
    Compound: 4, MMAE
    Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay
    Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay
    		[PMID: 25431858]
    MKN-45 IC50
    10.7 nM
    Compound: MMAE
    Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay
    Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay
    		[PMID: 35932567]
    NCI-H460 GI50
    0.683 nM
    Compound: 2b
    Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay
    		[PMID: 28211277]
    NCI-H460 GI50
    0.683 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
    Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
    		[PMID: 28926240]
    NCI-H460 GI50
    0.683 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
    Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
    		[PMID: 28895394]
    NCI-H524 IC50
    3.7 nM
    Compound: MMAE
    Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay
    Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay
    		[PMID: 30735385]
    NCI-N87 GI50
    0.54 nM
    Compound: 4, MMAE
    Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay
    Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay
    		[PMID: 25431858]
    NUGC-4 IC50
    10.97 nM
    Compound: MMAE
    Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay
    Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay
    		[PMID: 35932567]
    PC-3 CC50
    0.97 nM
    Compound: MMAE
    Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay
    Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay
    		[PMID: 34797052]
    SF-268 GI50
    0.432 nM
    Compound: 2b
    Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay
    		[PMID: 28211277]
    SF-268 GI50
    0.432 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human SF268 cells after 48 hrs by SRB assay
    Growth inhibition of human SF268 cells after 48 hrs by SRB assay
    		[PMID: 28926240]
    SF-268 GI50
    0.432 nM
    Compound: Desmethylauristatin E
    Growth inhibition of human SF268 cells after 48 hrs by SRB assay
    Growth inhibition of human SF268 cells after 48 hrs by SRB assay
    		[PMID: 28895394]
    SK-OV-3 IC50
    0.66 nM
    Compound: 2; MMAE
    Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay
    Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay
    		[PMID: 29454703]
    U-87MG ATCC EC50
    0.0002 μM
    Compound: Monomethyl auristatin E
    Antiproliferative activity against human U87 cells after 72 hrs by MTS assay
    Antiproliferative activity against human U87 cells after 72 hrs by MTS assay
    		[PMID: 28972755]
    體外研究
    (In Vitro)

    Monomethyl auristatin E (MMAE) 在 CD30+ 在癌細(xì)胞內(nèi)從 SGN-35 有效釋放，并且由于其膜滲透性，能夠?qū)χ車?xì)胞發(fā)揮細(xì)胞毒活性[1]。
    Monomethyl auristatin E (MMAE) 以與有絲分裂停滯相關(guān)的時(shí)間表和劑量依賴性的方式使結(jié)直腸癌細(xì)胞和胰腺癌細(xì)胞對(duì) IR 敏感。放射增敏作用表現(xiàn)為受照射細(xì)胞中克隆形成存活率下降和 DNA 雙鏈斷裂增加[2]。

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

    Monomethyl auristatin E (MMAE) 與 IR 結(jié)合導(dǎo)致腫瘤生長(zhǎng)延遲，腫瘤靶向 ACPP-cRGD-MMAE 與 IR 在異種移植模型中產(chǎn)生更穩(wěn)健并顯著延長(zhǎng)的腫瘤消退[2]。

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

    717.98

    Formula

    C39H67N5O7
    CAS 號(hào)
    性狀

    固體

    顏色

    White to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    -20°C, sealed storage, away from moisture and light

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    Ethanol 中的溶解度 : 50 mg/mL (69.64 mM; 超聲助溶)

    DMSO 中的溶解度 : ≥ 48 mg/mL (66.85 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.3928 mL 6.9640 mL 13.9280 mL
    5 mM 0.2786 mL 1.3928 mL 2.7856 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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    • 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.62 mg/mL (3.65 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.62 mg/mL (3.65 mM); 澄清溶液

    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

    只
    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）。

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    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: 99.97%

    參考文獻(xiàn)
    Cell Assay
    [2]

    Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. Thirty μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. Blots are developed by ECL.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system.

    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(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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 1.3928 mL 6.9640 mL 13.9280 mL 34.8199 mL
    5 mM 0.2786 mL 1.3928 mL 2.7856 mL 6.9640 mL
    10 mM 0.1393 mL 0.6964 mL 1.3928 mL 3.4820 mL
    15 mM 0.0929 mL 0.4643 mL 0.9285 mL 2.3213 mL
    20 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7410 mL
    25 mM 0.0557 mL 0.2786 mL 0.5571 mL 1.3928 mL
    30 mM 0.0464 mL 0.2321 mL 0.4643 mL 1.1607 mL
    40 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8705 mL
    50 mM 0.0279 mL 0.1393 mL 0.2786 mL 0.6964 mL
    60 mM 0.0232 mL 0.1161 mL 0.2321 mL 0.5803 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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