Monomethyl auristatin E

SKU: orb1300366

Description

Monomethyl auristatin E (MMAE) is a potent tubulin polymerization inhibitor that disrupts cell division. It serves as the cytotoxic payload in numerous antibody-drug conjugates (ADCs) and is widely used in oncology research for both in vitro cytotoxicity studies and in vivo xenograft models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 474645-27-7
• MW: 717.98
• Purity: 98.47% (May vary between batches)
• Formula: C₃₉H₆₇N₅O₇
• SMILES: CC[C@H](C)C([C@@H](CC(=O)N1CCC[C@H]1C(OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)[C@@H](C(C)C)C(=O)NC(=O)[C@@H](NC)C(C)C
• Target: Microtubule Associated|||ADC Cytotoxin|||Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.79 mM);DMSO:71.8 mg/mL (100 mM)

Bioactivity

• In Vivo:
  In the Karpas 299 ALCL model, cAC10-vcMonomethyl auristatin E (1 mg/kg, i.v.) induces complete, durable tumor regression, while free Monomethyl auristatin E (0.36 mg/kg) doesn't produce detectable antitumor activity. In mouse xenograft models of NHL, anti–CD79b-vcMonomethyl auristatin E (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission.
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• In Vitro:
  When coupled to cAC10, Monomethyl auristatin E shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. When coupled to anti-CD79b antibody, anti–CD79b-vcMonomethyl auristatin E has very potent and broad activity across a large panel of NHL cell lines in vitro. When coupled to anti-HER2 antibody, hertuzumab-vc-Monomethyl auristatin E can also be effectively internalized and potently kill HER2 over-expressing tumor cells.
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• Cell Research:
  Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT). (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Microtubule Associated, microtubule, MicrotubuleAssociated, Microtubule/Tubulin, MMAE, inhibit, Inhibitor, Monomethyl auristatin E, ADCCytotoxin, ADC Cytotoxin, ADC Payload, Apoptosis, SGD 1010, SGD1010, SGD-1010, Vedotin

Compound Identifiers

PubChem CID

126963463