中文同义词:
单甲基澳瑞他汀 D;一甲基澳瑞他汀 D;微管(TUBULIN)抑制剂(MMAD);一甲基澳瑞他汀D/MMAD/
英文名称:
MonoMethyl Dolastatin 10
英文同义词:
CS-1368;DEMETHYLDOLASTATIN 10; MONOMETHYLAURISTATIN D; MONOMETHYL DOLASTATIN 10;N-Methyl-L-valyl-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(2-thiazolyl)ethyl]amino]propyl]-1-pyrrolidinyl]-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide;EOS-60620;MMAD (Demethyldolastatin 10;Demethyldolastatin (MMAD);DeMethyldolastatin 10;MMAD
相关类别:
医药原料药;原料药【仅供科研】;细胞生物学试剂;科研原药系列;ADCs
沸点
906.1±65.0 °C(Predicted)
密度
1.119±0.06 g/cm3(Predicted)
储存条件
Sealed in dry,Store in freezer, under -20°C
酸度系数(pKa)
13.81±0.46(Predicted)
生物活性
MMAD 是一种有效的微管 (tubulin) 抑制剂，是抗体药物偶联物 (ADCs) 中的活性分子。
体外研究
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.
体内研究
The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats.
