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

VcMMAE 

Cat. No.: HY-15575 Purity: 99.89%
Data Sheet SDS Handling Instructions

VcMMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO $1173 In-stock
1 mg $260 In-stock
5 mg $520 In-stock
10 mg $810 In-stock
50 mg $2400 In-stock
100 mg   Get quote  
200 mg   Get quote  

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

    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

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    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].

    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].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [2]

    Monomethyl auristatin E is reconstituted in DMSO at a concentration of 5 nM.

    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
    Molecular Weight

    1316.63

    Formula

    C₆₈H₁₀₅N₁₁O₁₅

    CAS No.

    646502-53-6

    Storage

    4°C, protect from light, stored under nitrogen

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 54 mg/mL

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

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.89%

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