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)

Cat. No.: HY-15162 Purity: 99.75%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Monomethyl auristatin E Chemical Structure

Monomethyl auristatin E Chemical Structure

CAS No. : 474645-27-7

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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of Monomethyl auristatin E:

Top Publications Citing Use of Products

36 Publications Citing Use of MCE Monomethyl auristatin E

Proliferation Assay

    Monomethyl auristatin E purchased from MedChemExpress. 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    In Vitro

    Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1].
    MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[2].

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

    In Vivo

    Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models[2].

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

    Clinical Trial
    Molecular Weight

    717.98

    Formula

    C39H67N5O7

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC(C)[C@H](NC)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@@H](CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C)[C@H](C2=CC=CC=C2)O)=O)=O)OC)C)=O)C(C)C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    Ethanol : 50 mg/mL (69.64 mM; Need ultrasonic)

    DMSO : ≥ 48 mg/mL (66.85 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1393 mL 0.6964 mL 1.3928 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.62 mg/mL (3.65 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.62 mg/mL (3.65 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.48 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (3.48 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.48 mM); Clear solution

    • 6.

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.48 mM); Clear solution

    • 7.

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (3.48 mM); Clear solution

    • 8.

      Add each solvent one by one:  10% EtOH    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.48 mM); Clear solution

    • 9.

      Add each solvent one by one:  1% DMSO    99% Saline

      Solubility: ≥ 0.52 mg/mL (0.72 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

    References
    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.

    References
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    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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    Product Name:
    Monomethyl auristatin E
    Cat. No.:
    HY-15162
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