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VCMMAE

Catalog No. T4232   CAS 646502-53-6
Synonyms: mc-vc-PAB-MMAE

VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
VCMMAE Chemical Structure
VCMMAE, CAS 646502-53-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 48.00
10 mg In stock $ 91.00
25 mg In stock $ 166.00
50 mg In stock $ 265.00
100 mg In stock $ 397.00
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Purity: 100%
Purity: 99.58%
Purity: 99.27%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity.
In vitro MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, owing to its membrane permeability, it has the ability to exert cytotoxic activity on bystander cells. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells.
In vivo Monomethyl auristatin E (MMAE) in combination with IR results in increased DNA damage signaling and activation of CHK1 that delay the tumor growth. Tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models.
Cell Research 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. 30 μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies.
Animal Research 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.
Synonyms mc-vc-PAB-MMAE
Molecular Weight 1316.63
Formula C68H105N11O15
CAS No. 646502-53-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 54 mg/mL

TargetMolReferences and Literature

1. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinicalal Cancer Research (2010), 16(3), 888-897. 2. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87. 3. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library NO PAINS Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library

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Keywords

VCMMAE 646502-53-6 Cytoskeletal Signaling Microtubule Associated mc-vc-PAB-MMAE inhibit Drug-Linker Conjugates for ADC Inhibitor Microtubule/Tubulin inhibitor

 

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