Bavdegalutamide completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) < 1 nM.
Bavdegalutamide (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner.
Bavdegalutamide (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner.
Bavdegalutamide (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations.
Bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells.