D4-abiraterone

小分子

D4-阿比特龙

D4-abiraterone

D656087-1ml

1ml

10mM in DMSO

充氩,-80℃储存

超低温冰袋运输

D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1 , 3b-hydroxysteroid dehydrogenase ( 3βHSD ) and steroid-5a-reductase ( SRD5A ) and also an antagonist of androgen receptor . In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:CYP17A1, 3βHSD, SRD5A, androgen receptor

D4-阿比特龙是阿比特龙的主要代谢产物。D4-阿比特龙是 CYP17A1、3b-羟基类固醇脱氢酶（3βHSD）和类固醇-5a-还原酶（SRD5A）的抑制剂，也是雄激素受体的拮抗剂。

154229-21-7(DMSO)

C24H29NO

347.49 g/mol

CC12CCC(=O)C=C1CCC3C2CCC4(C3CC=C4C5=CN=CC=C5)C