Molecular Formula | C41H66N6O6S
|
Molar Mass | 771.06 |
Density | 1.119±0.06 g/cm3(Predicted) |
Boling Point | 906.1±65.0 °C(Predicted) |
pKa | 13.81±0.46(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Use | Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload and antibody drug conjugate. |
In vitro study | MMAD (Monomethyl Dolastatin 10) is coupled through a stable oxime-ligation process to yield several near-homogenous antibody-drug conjugates (ADCs) with a drug-to-antibody ratio of ~2.0. The resulting conjugates demonstrate good pharmacokinetic properties, potent in vitro cytotoxic activity against HER2+ cancer cells. When compared with ADCs prepared by cysteine alkylation following native interchain disulfide reduction, site-specific unnatural-amino-acid-based ADCs are shown to have increased in vitro cytotoxicity. |
In vivo study | The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats. |