中文名称:

恩杂鲁胺羧酸

中文同义词:

安扎鲁胺杂质M;安扎鲁胺杂质A;恩扎鲁安杂质A;恩杂鲁胺杂质A;恩杂鲁胺酸;恩杂鲁胺M1;恩杂鲁胺羧酸代谢物(M1);恩杂鲁胺羧酸

英文名称:

Enzalutamide carboxylic acid

英文同义词:

Desmethyl-enzalutamide;181240;Enzalutamide Carboxylic Acid Metabolite (M1);Enzalutamide impurity A;Enzalutamide Carboxylic Acid Metabolite;Enzalutamide Impurity M;4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluorobenzoic acid;Enzalutamide M1

CAS号:

1242137-15-0

分子式:

C20H13F4N3O3S

分子量:

451.39

EINECS号:

相关类别:

杂质对照品;恩杂鲁胺杂质

Mol文件:

1242137-15-0.mol

沸点 

590.2±60.0 °C(Predicted)

密度 

1.59±0.1 g/cm3(Predicted)

储存条件 

Sealed in dry,2-8°C

酸度系数(pKa)

2.94±0.10(Predicted)

用途

恩杂鲁胺羧酸为羧酸胺类有机物，可用作杂质对照品。

生物活性

Enzalutamide carboxylic acid (MDV3100 carboxylic acid) 是 Enzalutamide (MDV3100) 的非活性代谢产物。Enzalutamide 是雄激素受体 (AR) 拮抗剂。

体外研究

Enzalutamide is converted into its major metabolites, N-desmethyl enzalutamide and carboxylic acid enzalutamide, by cytochrome P450 (CYP) 3A4/5 and CYP2C8, respectively. N-desmethyl enzalutamide has clinically relevant anti-androgen capacities similar to enzalutamide, whereas carboxylic acid enzalutamide is inactive.