Fig. 2

Efficacy and IC50s to block endogenous expression of genes transcriptionally regulated by full-length AR. a LNCaP xenografts grown in castrated mice dosed by gavage daily with vehicle (VEH), BU27 (30 mg/kg), its matching analogue BU3-12 (30 mg/kg), and enzalutamide (10 mg/kg). b LNCaP xenografts grown in castrated mice dosed by gavage daily with vehicle (VEH), BU130 (30 mg/kg), its matching analogue BU170 (30 mg/kg), and enzalutamide (10 mg/kg). c mRNA levels of androgen-induced genes normalized to housekeeping gene SDHA from LNCaP cells. Data presented as mean ± SEM and normalized to DMSO vehicle control in presence of R1881 (n = 3 independent experiments). d Table showing IC50 values for each inhibitor for genes shown in c. The sum-of-squares F test was performed to compare IC50’s for each inhibitor against EPI-002 (ralaniten). e Transcript levels of androgen-repressed genes normalized to levels of housekeeping gene SDHA from LNCaP cells treated as in c. Data presented as mean ± SEM, and analyzed by one-way ANOVA with Dunnet’s correction (n = 3 independent experiments). ND: not detected. *p < 0.05; **p < 0.01; ***p < 0.001; ****p < 0.0001