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

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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  • Biological Activity

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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
NCT Number Sponsor Condition Start Date Phase
NCT00412828 CuraGen Corporation|Celldex Therapeutics Unresectable Stage III or Stage IV Melanoma June 2006 Phase 1|Phase 2
NCT00704158 CuraGen Corporation|Celldex Therapeutics Breast Cancer June 2008 Phase 1|Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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
M.Wt

1316.63

Formula

C₆₈H₁₀₅N₁₁O₁₅

CAS No.

646502-53-6

Storage

Powder4°C, protect from light, stored under nitrogen

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 54 mg/mL

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

Purity: 99.89%

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VcMMAE
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