中文名 | 17-(3-pyridyl)androsta-5,16-dien-3-one |
英文名 | 17-(3-pyridyl)androsta-5,16-dien-3-one |
别名 | 松香酮杂质41 阿比特龙代谢物 阿比特龙杂质41 醋酸阿比特龙杂质19 17-(3-吡啶基)-雄甾-4,16-二烯-3-酮 |
英文别名 | D4-abiraterone Δ4-Abiraterone Abiraterone (D4A) D4-abiraterone (CB-7627) 7-(3-pyridyl)androsta-5,16-dien-3-one 17-(3-pyridyl)androsta-5,16-dien-3-one 17-(3-pyridinyl)-androsta-4,16-diene-3-one |
CAS | 154229-21-7 |
化学式 | C24H29NO |
分子量 | 347.49 |
密度 | 1.14±0.1 g/cm3(Predicted) |
沸点 | 504.6±50.0 °C(Predicted) |
酸度系数 | 5.32±0.12(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.878 ml | 14.389 ml | 28.778 ml |
5 mM | 0.576 ml | 2.878 ml | 5.756 ml |
10 mM | 0.288 ml | 1.439 ml | 2.878 ml |
5 mM | 0.058 ml | 0.288 ml | 0.576 ml |
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