Abiraterone Acetate,154229-18-2

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YZ剂描述：

产品名称：Abiraterone Acetate

产品别名：乙酸阿比特龙酯

英文别名：CB7630

靶点：CYP17

CAS：154229-18-2

纯度：>98%

外观：白色至类白色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Abiraterone Acetate (CB 7630) is a highly active and selective 17α-hydroxylase/17,20 lyase (CYP17A1) inhibitor with an IC50 of 72 nM. Abiraterone Acetate (CB 7630) inhibitor CYP11B1, CYP11B2 and CYP3A4 with IC50 of 1.6, 1.8 and 2.7 μM. Abiraterone Acetate (CB 7630) is used in the study of castration-resistant prostate cancer. Abiraterone Acetate (CB 7630) blocks the formation of testosterone by inhibiting CYP17A1. Abiraterone Acetate (CB 7630) caused significant reductions in the weights of the ventral prostate and seminal vesicles. There was no reduction seen in the weight of these organs with KC. Abiraterone Acetate (CB 7630) reduced plasma testosterone to 0.1 nM or less, despite a three- to four-fold increase in the plasma level of luteinizing hormone (LH).

溶解性：Ethanol ：27 mg/mL (69 mM)

体外研究：

Abiraterone shows a good complexation with the heme iron only in SM1. Abiraterone blocks the synthesis of androgens by inhibiting CYP17A1. Abiraterone also blocks 3β-hydroxysteroid dehydrogenase (3βHSD), an enzyme that is absolutely required for the synthesis of biologically active androgens. Abiraterone inhibits conversion of DHEA to Δ4-androstenedione. Abiraterone inhibition of 3βHSD blocks DHT synthesis and the androgen receptor response. Abiraterone inhibits the conversion of Δ5-androstenediol to testosterone. Abiraterone inhibits C17,20-lyase, with an IC50 of 5.8 nM, in rat testis microsomes. Abiraterone significantly inhibits testosterone secretion (−48%) and in turn increases LH concentration (192%). Abiraterone inhibits in vitro proliferation and AR-regulated gene expression of AR-positive prostate cancer cells, which could be explained by AR antagonism in addition to inhibition of steroidogenesis.

体内研究：Following intraperitoneal administration in a rodent model, abiraterone was found to have rapid deacetylation. When administered as its acetate pro-drug (CB 7630), it suppressed circulating testosterone to undetectable levels and markedly decreased the weights of androgen sensitive organs. Abiraterone is well tolerated and the mean elimination half-life of abiraterone in these studies was 27.6 h (thus supporting the use of once-daily dosing). Preclinical studies with abiraterone demonstrated reduction in androgen production downstream of CYP17 which resulted in decreased weight of the ventral prostate, testis, and seminal vesicles in mice.

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