Abiraterone 154229-19-3

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Molecular Weight:

349.51 Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM.

Biological Activity

Abiraterone binds and inhibits wild-type and mutant androgen receptor
(AR). Abiraterone inhibits in vitro proliferation and androgen
receptor-regulated gene expression of androgen receptor-positive
prostate cancer cells, which could be explained by androgen receptor
antagonism in addition to inhibition of steroidogenesis. In fact,
activation of mutant androgen receptor by eplerenone is inhibited by
greater concentrations of Abiraterone.


Abiraterone displaces ligand from
both WT-AR and T877A with EC50 of 13.4 μM and 7.9 μM, respectively. Abiraterone
inhibits lyase activity with an IC50 of 5.8 nM in rat testis
microsomes. Abiraterone acetate significantly inhibits T secretion
(−48%) and in turn increased LH concentration (192%).


Abiraterone inhibits CYP17 with an IC50 of 72 nM, in human testicular microsomes. Abiraterone fails to significantly reduce the size of any of the organs. Abiraterone reduces the testosterone levels strongly, almost reaching
the level of the orchiectomy control. The testosterone levels are
reduced by Abiraterone for more than 95% compared to the control group.

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Product Categories : Metabolism > P450 Inhibitor