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Chemical Structure : ARD-69
CAS No.: 2316837-10-0
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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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.
| M.Wt | 1129.82 | |
| Formula | C62H74ClFN8O7S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Xin Han, et al. J Med Chem. 2019 Jan 24;62(2):941-964.
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