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Description: Bicalutamide (also known as ICI-176334; CDX; trade names: Casodex in the USA and Cosudex in other countries), a marketed drug for treating PC (prostate cancer), is a potent, synthetic, nonsteroidal androgen receptor (AR) antagonist with IC50 of 0.16 uM in LNCaP/AR(cs)cell line. Bicalutamide inhibits the growth of prostate cancer cells which overexpress androgen receptor by directly binding to AR then mediates androgen-mediated gene transcription. Bicalutamide directly binds to androgen receptor with Ki value of 12.5uM. In prostate cancer cells, bicalutamide impairs DNA binding and nuclear localization. Bicalutamide and MDV3100 significantly inhibited R1881-induced VP16-AR–mediated transcription in HepG2 cells with an IC50 value of 0.2 uM.
References: Cancer Res. 2012 Mar 15; 72(6):1494-503; Int J Oncol. 2012 Aug; 41(2):425-32.
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