1. Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage Cytoskeleton
  2. Drug-Linker Conjugates for ADC Microtubule/Tubulin
  3. VcMMAE

VcMMAE  (Synonyms: MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE)

Cat. No.: HY-15575 Purity: 99.90%
COA Handling Instructions

VcMMAE (mc-vc-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

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

VcMMAE Chemical Structure

VcMMAE Chemical Structure

CAS No. : 646502-53-6

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Customer Review

Based on 40 publication(s) in Google Scholar

Other Forms of VcMMAE:

Top Publications Citing Use of Products

39 Publications Citing Use of MCE VcMMAE

Proliferation Assay

    VcMMAE purchased from MedChemExpress. Usage Cited in: Exp Biol Med (Maywood). 2017 Aug;242(14):1405-1411.  [Abstract]

    Cell viability assay. Alamar Blue cell viability assay of Karpas 299 cells after 72 hours of treatment with vcMMAE (purple) and TMV-vcMMAE (blue) at 0.02 nM to 200 nM vcMMAE; non-conjugated TMV is also tested using the protein concentration corresponding to the highest vcMMAE dose (200 nM), toxicity of TMV is not observed.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    VcMMAE (mc-vc-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

    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 sensitized 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 prolonged tumor regression in xenograft models[2].

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

    Molecular Weight

    1316.63

    Appearance

    Solid

    Formula

    C68H105N11O15

    CAS No.
    SMILES

    CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(COC(N(C)[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N2[C@@]([C@H](OC)[C@@H](C)C(N[C@H](C)[C@@H](O)C3=CC=CC=C3)=O)([H])CCC2)=O)C)=O)=O)=O)C=C1)=O)=O)NC(CCCCCN4C(C=CC4=O)=O)=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: 

    DMSO : ≥ 54 mg/mL (41.01 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 0.7595 mL 3.7976 mL 7.5951 mL
    5 mM 0.1519 mL 0.7595 mL 1.5190 mL
    10 mM 0.0760 mL 0.3798 mL 0.7595 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      VcMMAE is dissolved in DMSO and then diluted with 0.9% NaCl[3].

    Purity & Documentation

    Purity: 99.90%

    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. 30μg 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]

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

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    Product Name:
    VcMMAE
    Cat. No.:
    HY-15575
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