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Chemical Structure : ARD-2051
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.
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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.
| M.Wt | 789.33 | |
| Formula | C43H45ClN8O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xin Han, et al. J Med Chem. 2023 Jul 13;66(13):8822-8843.
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