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ARD-69

Chemical Structure : ARD-69

CAS No.: 2316837-10-0

ARD-69 (ARD69)

Catalog No.: PC-49044Not For Human Use, Lab Use Only.

ARD-69 is a highly potent PROTAC degrader of androgen receptor (AR), effectively induces degradation of AR protein in AR-positive prostate cancer cell lines LNCaP, VCaP, and 22Rv1 with DC50 values of 0.86, 0.76, and 10.4 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ARD-69 is a highly potent PROTAC degrader of androgen receptor (AR), effectively induces degradation of AR protein in AR-positive prostate cancer cell lines LNCaP, VCaP, and 22Rv1 with DC50 values of 0.86, 0.76, and 10.4 nM, respectively.
ARD-69 is capable of reducing the AR protein level by >95% in these prostate cancer cell lines and effectively suppressing AR-regulated gene expression.
ARD-69 potently inhibits cell growth in AR-positive prostate cancer cell lines and is >100 times more potent than AR antagonists.
ARD-69 effectively reduces the level of AR protein in xenograft tumor tissue in mice.

Physicochemical Properties

M.Wt 1129.82
Formula C62H74ClFN8O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-N-((S)-3-(4-((4-(((1r,3r)-3-(3-Chloro-4-cyanophenoxy)- 2,2,4,4-tetramethyl-cyclobutyl)carbamoyl)phenyl)ethynyl)-[1,4'-bipiperidin]-1'-yl)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)-1- ((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide

References

1. Xin Han, et al. J Med Chem. 2019 Jan 24;62(2):941-964.

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