UT-155

**UT-155** is a selective and potent small molecule antagonist and degrader of the androgen receptor (AR), with a binding affinity (Ki) of 267 nM to the AR ligand-binding domain (AR-LBD). Developed through medicinal chemistry optimization, it exhibits 6-10-fold higher potency than enzalutamide in inhibiting R1881-induced wild-type AR transactivation and maintains efficacy against mutant ARs (e.g., W742L), where enzalutamide is less effective. In prostate cancer models like LNCaP and 22RV1 cells/xenografts, UT-155 potently suppresses AR-dependent gene expression (PSA, FKBP5), AR splice variants (AR-V7), and tumor growth (53% inhibition in 22RV1 xenografts), outperforming enzalutamide in enzalutamide-resistant settings via proteasome-mediated AR degradation.[1][2][7]

Other names

(S)-UT-155