单甲基澳瑞他汀 D
| 中文名称 | 单甲基澳瑞他汀 D |
|---|---|
| 中文同义词 | 单甲基澳瑞他汀 D;一甲基澳瑞他汀 D;一甲基澳瑞他汀D/MMAD/;微管(TUBULIN)抑制剂(MMAD);MMAD游离态;(S)-N-((3R,4S,5S)-3-甲氧基-1-((S)-2-((1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(((S)-2-苯基-1-(噻唑-2-基)乙基)氨基)丙基)吡咯烷-1-基)-5-甲基-1-氧代庚-4-基)-N,3-二甲基-2-((S)-3-甲基-2-(甲基氨基)丁酰胺基)丁酰胺 |
| 英文名称 | MonoMethyl Dolastatin 10 |
| 英文同义词 | 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;DeMethyldolastatin 10;MMAD;MonoMethyl Dolastatin 10;MonoMethylauristatin D;(S)-N-((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide;CS-1368;DEMETHYLDOLASTATIN 10; MONOMETHYLAURISTATIN D; MONOMETHYL DOLASTATIN 10 |
| CAS号 | 203849-91-6 |
| 分子式 | C41H66N6O6S |
| 分子量 | 771.06 |
| EINECS号 | |
| 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;化学试剂;ADCs |
| Mol文件 | 203849-91-6.mol |
| 结构式 |  |
单甲基澳瑞他汀 D 性质
| 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 |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 13.81±0.46(Predicted) |
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。
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Auristatin
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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.
The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15581 | 单甲基澳瑞他汀 D MMAD | 203849-91-6 | 5mg | 800元 |
| 2024/01/25 | HY-15581 | 单甲基澳瑞他汀 D MMAD | 203849-91-6 | 10mg | 1400元 |