阿比特龙代谢物
中文名称 | 阿比特龙代谢物 |
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中文同义词 | 阿比特龙代谢物;松香酮杂质41;醋酸阿比特龙杂质19;17-(3-吡啶基)-雄甾-4,16-二烯-3-酮;阿比特龙杂质41;2H4]-DELTA 4-阿比特龙;阿比特龙杂质59;ABIRATERONE D4A METABOLITE|||CB-7627|||Δ4-ABIRATERONE |
英文名称 | 17-(3-pyridyl)androsta-5,16-dien-3-one |
英文同义词 | 17-(3-pyridyl)androsta-5,16-dien-3-one;7-(3-pyridyl)androsta-5,16-dien-3-one;17-(3-pyridinyl)-androsta-4,16-diene-3-one;D4-abiraterone (CB-7627);D4-abiraterone;Abiraterone 3-Oxo 4,5-Dihydro Impurity/(8R,9S,10R,13S,14S)-10,13-Dimethyl-17-(pyridin-3-yl)-1,7,8,9,10,11,12,13,14,15-decahydro-2H-cyclopenta[a]phenanthren-3(6H)-one;Abiraterone (D4A);Δ4-Abiraterone |
CAS号 | 154229-21-7 |
分子式 | C24H29NO |
分子量 | 347.49 |
EINECS号 | |
相关类别 | 142-醋酸阿比特龙 |
Mol文件 | 154229-21-7.mol |
结构式 | ![]() |
阿比特龙代谢物 性质
沸点 | 504.6±50.0 °C(Predicted) |
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密度 | 1.14±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:10mg/mL |
形态 | 粉末 |
酸度系数(pKa) | 5.32±0.12(Predicted) |
颜色 | 白色至米色 |
CYP17A1, 3βHSD, SRD5A, androgen receptor
D4-abiraterone (D4A ) (10 mM) nearly completely blocks conversion from D4-androstenedione (AD) to 5α-androstanedione and other 5α-reduced androgens. The affinity of D4-abiraterone for mutant (expressed in LNCaP, half-maximum inhibitory concentration (IC 50 =5.3 nM)) and wild type (expressed in LAPC4, IC 50 =7.9 nM) androgen receptor (AR) is greater than that of abiraterone (Abi) (IC 50 =418 and >500 nM, respectively). Compare with Abi, D4-abiraterone clearly better suppresses PSA, TMPRSS2 and FKBP5 expression in LNCAP, LAPC4 and C4-2 cell lines. D4-abiraterone also inhibits AR target gene expression in a dose-dependent manner.
D4-abiraterone (D4A) is tenfold more potent than abiraterone (Abi) in blocking conversion from dehydroepiandrosterone (DHEA) by 3β-hydroxysteroid dehydrogenase (3βHSD) to D4-androstenedione (AD) in LNCaP and VCaP xenografts. 0.1 μM D4-abiraterone is equivalent to 1 μM Abi for blocking AD accumulation at 48 h in both LNCaP and VCaP xenografts. Progression is significantly delayed in the D4-abiraterone group compare with the Abi acetate group (P=0.011). D4-abiraterone treatment increases progression-free survival compare with Abi acetate.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-109619 | 阿比特龙代谢物 D4-abiraterone | 154229-21-7 | 5mg | 2800元 |
2024/04/30 | HY-109619 | 阿比特龙代谢物 D4-abiraterone | 154229-21-7 | 10mM * 1mLin DMSO | 3080元 |