ARD-2051 | AR PROTAC | Probechem Biochemicals

Chemical Structure : ARD-2051

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ARD-2051 (ARD2051, ARD 2051)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	789.33
分子式	C43H45ClN8O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Chloro-4-((3S)-8-(4-(4-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)azetidin-3-yl)piperazine-1-carbonyl)phenyl)-3-methyl-2,8-diazaspiro[4.5]decan-2-yl)benzonitrile

参考文献

1. Xin Han, et al. J Med Chem. 2023 Jul 13;66(13):8822-8843.

ARD-2051 (ARD2051, ARD 2051)

生物&药学活性

物理化学性质&存储条件

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ARD-2051 (ARD2051, ARD 2051)

生物&药学活性

物理化学性质&存储条件

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