Monomethyl auristatin E (MMAE; Vedotin) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. Monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc). Antibody-drug conjugates (ADCs) are designed to combine the exquisite specificity of antibodies to target tumor antigens with the cytotoxic potency of chemotherapeutic drugs. In vivo studies demonstrated that the peptide-linked conjugates induced regressions and cures of established tumor xenografts with therapeutic indices as high as 60-fold.*The compound is unstable in solutions, freshly prepared is recommended
| Cell Experiment | |
|---|---|
| Cell lines | CD30+ Karpas 299 cells |
| Preparation method | Using Alamar Blue dye reduction assay to measure cytotoxicity according to the manufacturer's directions. Briefly, freshly preparing a 40% solution (wt/vol) of Alamar Blue in complete media just before adding cultures . Ninety-two hours after drug exposure, adding Alamar Blue solution to cells to constitute 10% culture volume. Incubating cells for 4 hours, and measuring dye reduction on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT). |
| Concentrations | ~1000 ng/mL |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID mice bearing Karpas 299 (ALCL) or L540cy (HD) tumors |
| Formulation | |
| Dosages | 0.36 mg/kg |
| Administration | i.v. |
| Molecular Weight | 717.98 |
| Formula | C39H67N5O7 |
| CAS Number | 474645-27-7 |
| Solubility (25°C) | DMSO >48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Marie Alt, et al. Enfortumab Vedotin in urothelial cancer
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