ARD-266 |
| Catalog No.GC60595 |
L'ARD-266 est un dégradeur PROTAC très puissant et basé sur la ligase E3 de von Hippel-Lindau. L'ARD-266 induit efficacement la dégradation de la protéine AR dans les lignées cellulaires de cancer de la prostate LNCaP, VCaP et 22Rv1 positives pour AR avec des valeurs DC50 de 0,2 À 1 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM[1].
ARD-266 (Compound 11; 100 nM; 1-24 hours; LNCaP and VCaP cells) treatment effectively reduces the AR protein level within 3 h and achieves near-complete AR elimination with a 6 h treatment in the LNCaP cells[1].ARD-266 (Compound 11; 1-10000 nM; 24 hours; LNCaP cells) treatment effectively suppresses the expression of PSA, TMPRSS2, and FKBP5 genes in a dosedependent manner and is capable of reducing the mRNA levels of PSA, TMPRSS2, and FKBP5 genes by >50% at 10 nM in the LNCaP cell line[1]. Western Blot Analysis[1] Cell Line: LNCaP and VCaP cells
[1]. Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231.
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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