VCMMAE

SKU: orb1303037

Description

VCMMAE

Research Area

Signal Transduction

Key Properties

• CAS Number: 646502-53-6
• MW: 1316.63
• Purity: 99.56%
• Formula: C₆₈H₁₀₅N₁₁O₁₅
• SMILES: CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)C=CC2=O)C(C)C)cc1)C(C)C
• Target: Drug-Linker Conjugates for ADC,Microtubule Associated
• Solubility: DMSO:62.5 mg/mL (47.47 mM)

Bioactivity

• In Vivo:
  Monomethyl auristatin E (MMAE), when combined with IR, enhances DNA damage signaling and CHK1 activation, delaying tumor growth. Tumor-targeted ACPP-cRGD-MMAE with IR induces more robust and significantly prolonged tumor regression in xenograft models.
• 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 ha the ability to exert cytotoxic activity on bys ander cells. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double st and breaks in irradiated cells.
• 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 f Male athymic nu/nu mice are injected Subcutaneously into thighs with × 06 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 wit the UltraMap system.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Microtubule Associated, Microtubule/Tubulin, MicrotubuleAssociated, inhibit, Inhibitor, mc-vc-PAB-MMAE, Drug-Linker Conjugates for ADC, DrugLinker Conjugates for ADC, DrugLinkerConjugatesforADC, VCMMAE

Compound Identifiers

PubChem CID

46944733