UT-155

UT-155 是一种选择性的、有效的雄激素受体 (AR) 拮抗剂，与 AR-LBD 结合的 K_i 值为 267 nM。UT-155 binds to the AR-LBD at K_i of 267 nM. UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide is weaker by two fold with the W742L mutant AR relative to the wild type AR. Treatment of LNCaP cells with UT-155 inhibits 0.1 nM R1881-induced PSA and FKBP5 gene expression between 10 and 100 nM with 5-10-fold better potency than enzalutamide