Conditionnement : 10mg
Téléphone : +1 850 650 7790
Synonyms: Vedotin, MMAE
| 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. |
| 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] |
| Synonyms | Vedotin, MMAE |
| 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) |
| Molecular Weight | 717.98 |
| Formula | C39H67N5O7 |
| Cas No. | 474645-27-7 |
| 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 |
| Relative Density. | 1.088 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (139.28 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.79 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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