ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.

VCaP cells:1.5 nM, LNCaP AR+ cell:16.2 nM

ARD-2585 is effective in reducing the AR protein level at the 3 and 24 h time-points by 78% and 60% at the 6 h time-point. ARD-2585 achieves picomolar DC50 values and >98% of Dmax in the VCaP cell line with a wild-type AR and in the LNCaP cell line carrying a T878A-mutated AR mutant. ARD-2585 potently inhibits cell growth with IC50 values of 1.5 nM and 16.2 nM in the VCaP and LNCaP AR+ prostate cancer cell lines. [1]

At the end of the treatment (day 37), 20 and 40 mg/kg ARD-2585 inhibits tumor growth by 54.9, 74.3, and 65.9%. ARD-2585 effectively reduces AR protein the VCaP xenograft tumor tissue in mice and inhibits VCaP tumor growth. [1]