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154229-21-7

中文名稱 阿比特龍代謝物
CAS 154229-21-7
分子式 C24H29NO
分子量 347.49
MOL 文件 154229-21-7.mol
更新日期 2023/04/19 08:56:48
154229-21-7 結(jié)構(gòu)式 154229-21-7 結(jié)構(gòu)式

基本信息

中文別名
阿比特龍代謝物
英文別名
CB-7627
D4-abiraterone
Δ4-Abiraterone
Abiraterone (D4A)
Delta 4-Abiraterone
Abiraterone Impurity 59
D4-abiraterone (CB-7627)
Abiraterone D4A metabolite
7-(3-pyridyl)androsta-5,16-dien-3-one
17-(3-pyridyl)androsta-5,16-dien-3-one

物理化學(xué)性質(zhì)

沸點504.6±50.0 °C(Predicted)
密度1.14±0.1 g/cm3(Predicted)
儲存條件2-8°C
酸度系數(shù)(pKa)5.32±0.12(Predicted)
形態(tài)粉末
顏色白色至米色
阿比特龍代謝物價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-109619阿比特龍代謝物
D4-abiraterone
154229-21-75mg1390元
2024/11/08HY-109619阿比特龍代謝物
D4-abiraterone
154229-21-710mM * 1mLin DMSO1529元
2024/11/08HY-109619阿比特龍代謝物
D4-abiraterone
154229-21-710mg2232元

常見問題列表

生物活性
D4-abiraterone 是阿比特龍的主要代謝產(chǎn)物。D4-abiraterone 是 CYP17A1, 3β-羥基類固醇脫氫酶 (3 βHSD) 和類固醇-5α-還原酶 ( SRD5A ) 的抑制劑,也是雄激素受體的拮抗劑。
靶點

CYP17A1, 3βHSD, SRD5A, androgen receptor

體外研究

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.

體內(nèi)研究

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.

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