MMAD 是一种有效的微管蛋白抑制剂，是抗体药物偶联物中的一种毒素有效载荷。

MMAD is a potent tubulin inhibitor. MMAD is a toxin payload in antibody drug conjugates (ADCs).

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. The site-specific unnatural-amino-acid-based ADCs are shown to have increased in vitro cytotoxicity when compared with ADCs prepared by cysteine alkylation following native interchain disulfide reduction.

The resulting antibody-drug conjugates (ADCs) exhibited complete tumor regression in rodents. They also have an improved toxicology profile in rats.

203849-91-6

C41H66N6O6S

771.08

Demethyldolastatin 10;Monomethylauristatin D;Monomethyl Dolastatin 10;单甲基澳瑞他汀 D

DMSO:24.5 mg/mL (31.77 mM)),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years