| Description | D8-MMAF is a microtubule destroyer, deuterated form of MMAF. |
| In vitro | MMAF showed cytotoxicity in vitro against a group of cell lines. Karpas 299, H3396, 786-O and Caki-1 have IC50 values of 119, 105, 257 and 200 nM, respectively. Targeted MMAF is more effective than free drug, and the cAC10 conjugate of MMAF shows significant activity. On a molar basis, the average potency of cAC10-L1-MMAF4 is more than 2200 times higher than free MMAF, and it is active in all tested CD30 positive cell lines. |
| In vivo | The maximum tolerated dose of MMAF (> 16 mg / kg) mice is much higher than that of MMAE (1 mg / kg). The MTD of cAC10-L1-MMAF4 is 50 mg / kg in mice and 15 mg / kg in rats. The corresponding cAC10-L4-MMAF4 ADC is much less toxic, with MTD greater than 150 mg / kg and 90 mg / kg in mice and rats, respectively. |
| Synonyms | Monomethylauristatin F D8 |
| molecular weight | 740.01 |
| Molecular formula | C39H57D8N5O8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24. |