ARD-266是一种高效且基于VHLE3连接酶的雄激素受体(androgenreceptor,AR)PROTAC降解剂。ARD-266有效诱导AR阳性LNCaP，VCaP和22Rv1前列腺癌细胞系中AR蛋白的降解，DC50值为0.2-1nM。
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.
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