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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

Images & Validation

Key Properties

CAS Number474645-27-7
MW717.98
Purity99.90%
FormulaC39H67N5O7
SMILESCC[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
TargetApoptosis,ADC Cytotoxin,Microtubule Associated
Solubility10% 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.
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.
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)

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor 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

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Key Properties

No computed properties available.

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Monomethyl auristatin E (orb1300366)

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10 mg
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25 mg
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50 mg
$ 140.00
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