| Name | Monomethyl auristatin E |
| Description | Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity. |
| 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) |
| 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. [1] 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. [2] When coupled to anti-HER2 antibody, hertuzumab-vc-Monomethyl auristatin E can also be effectively internalized and potently kill HER2 over-expressing tumor cells. [3] |
| 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. [1] In mouse xenograft models of NHL, anti–CD79b-vcMonomethyl auristatin E (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission. [2] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 71.8 mg/mL (100 mM)
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| Keywords | SGD1010 | Monomethyl auristatin E | Microtubule/Tubulin | SGD 1010 | Apoptosis | inhibit | SGD-1010 | Inhibitor | ADC Payload | ADC Cytotoxin |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin |
United States
