中文名 | MMAD |
英文名 | MMAD |
别名 | MMAD游离态 单甲基澳瑞他汀 D 一甲基澳瑞他汀 D 微管(TUBULIN)抑制剂(MMAD) |
英文别名 | MMAD CS-1368 EOS-60620 DEMETHYLDOLASTATIN 10 DeMethyldolastatin 10 MONOMETHYLAURISTATIN D Demethyldolastatin (MMAD) MONOMETHYL DOLASTATIN 10 MMAD (Demethyldolastatin 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 |
CAS | 203849-91-6 |
化学式 | C41H66N6O6S |
分子量 | 771.06 |
密度 | 1.119±0.06 g/cm3(Predicted) |
沸点 | 906.1±65.0 °C(Predicted) |
酸度系数 | 13.81±0.46(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.297 ml | 6.485 ml | 12.969 ml |
5 mM | 0.259 ml | 1.297 ml | 2.594 ml |
10 mM | 0.13 ml | 0.648 ml | 1.297 ml |
5 mM | 0.026 ml | 0.13 ml | 0.259 ml |
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