Catalog No.: PC-21161Not For Human Use, Lab Use Only.
ARD-2051 (ARD-2051) is a potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera (PROTAC) degrader with DC50 of 0.6 nM in AR+ VCaP and LNCaP cell lines.
ARD-2051 (ARD-2051) is a potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera (PROTAC) degrader with DC50 of 0.6 nM in AR+ VCaP and LNCaP cell lines.
ARD-2051 shows Dmax >90% in inducing AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines, potently and effectively suppresses AR-regulated genes, and inhibits cancer cell growth (VCaP and LNCaP, IC50=10 and 13 nM, respectively).
ARD-2051 (12.5 mg/kg) strongly reduces AR protein and suppresses AR-regulated gene expression in the VCaP xenograft tumor tissue in mice.
ARD-2051 (3.75, 7.5, 15, and 30 mg/kg) effectively inhibited tumor growth in the VCaP xenograft tumor model in SCID mice.
