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

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

目录号: HY-15162 纯度: 99.97%
COA 产品使用指南

Monomethyl auristatin E (MMAE; SGD-1010) 是海兔毒素 10 的合成衍生物,通过抑制微管蛋白聚合而起到有效的有丝分裂抑制作用。 MMAE 广泛用作细胞毒性成分制作抗体偶联活性分子 (ADCs) 用于癌症的研究。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Monomethyl auristatin E Chemical Structure

Monomethyl auristatin E Chemical Structure

CAS No. : 474645-27-7

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Customer Review

Other Forms of Monomethyl auristatin E:

MCE 顾客使用本产品发表的 40 篇科研文献

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

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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

     

    细胞效力
    (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]
    体外研究
    (In Vitro)

    单甲基 auristatin E (MMAE) 在 CD30+ 在癌细胞内从 SGN-35 有效释放,并且由于其膜渗透性,能够对周围细胞发挥细胞毒活性[1]
    MMAE 以与有丝分裂停滞相关的时间表和剂量依赖性的方式使结直肠癌细胞和胰腺癌细胞对 IR 敏感。放射增敏作用表现为受照射细胞中克隆形成存活率下降和 DNA 双链断裂增加[2]

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

    体内研究
    (In Vivo)

    单甲基 auristatin E (MMAE) 与 IR 结合导致肿瘤生长延迟,肿瘤靶向 ACPP-cRGD-MMAE 与 IR 在异种移植模型中产生更稳健并显著延长的肿瘤消退[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 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

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

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    溶解性数据
    细胞实验: 

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

    DMSO 中的溶解度 : ≥ 48 mg/mL (66.85 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

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

      Solubility: 2.62 mg/mL (3.65 mM); 澄清溶液; 超声助溶

    • 方案 二

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in Saline)

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

    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

    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)。

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    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: 99.97%

    参考文献
    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.

    参考文献

    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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    可选溶剂 浓度 溶剂体积 质量 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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