ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor[1].
ARD-2585 achieves DC50 values of 0.04-0.1 nM in the VCaP cell line with AR gene amplification and in the LNCaP cell line carrying an AR mutation[1].ARD-2585 (100 nM) is effective in reducing the AR protein level at the 3 and 24 h time-points by 78% (p 0.05)[1].
[1]. Weiguo Xiang. et al. Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2021 Sep 23;64(18):13487-13509.