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: 99.27%
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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Top Publications Citing Use of Products
  • 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].

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.

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.

References
M.Wt

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

Purity: 99.27%

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