| Description | D8-MMAD is a deuterated form of MMAD, which is a microtubule destroyer. |
| In vitro | MMAD (monomethyl Dolastatin 10) is coupled through a stable oxime ligation process to produce several nearly uniform antibody-drug conjugates (ADC) with a pharmacodynamic ratio of approximately 2.0. The resulting conjugate showed good pharmacokinetic properties and had strong in vitro cytotoxic activity against HER2 + cancer cells. Compared with ADCs prepared by cysteine alkylation after reduction of natural interchain disulfide bonds, site-based unnatural amino acid-based ADCs have higher cytotoxicity in vitro. |
| In vivo | The resulting antibody-drug conjugate (ADC) showed complete tumor regression in rodents. Their toxicological characteristics in rats have also been improved. |
| Synonyms | Monomethylauristatin D D8, Demethyldolastatin 10 D8, Monomethyl Dolastatin 10 D8 |
| molecular weight | 779.11 |
| Molecular formula | C41H58D8N6O6S |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (128.35 mM) |
| References | 1. Chudasama V, et al. Recent advances in the construction of antibody-drug conjugates. Nat Chem. 2016 Feb;8(2):114-9. |