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ARD-61

CAS No. : 2316837-08-6

MCE 站：ARD-61

产品活性：ARD-61 是一种高效、特异的 PROTAC 雄激素受体 (AR) 降解剂。ARD-61 有效且有效地诱导 AR+ 癌细胞系中的 AR 和孕酮受体 (PR) 降解。ARD-61 诱导细胞凋亡，也可有效抑制小鼠 MDA-MB-453 异种移植模型中的肿瘤生长。

研究领域：PROTAC  |  Others  |  Apoptosis

作用靶点：PROTACs  |  Androgen Receptor  |  Progesterone Receptor  |  Apoptosis

In Vitro: ARD-61 binds to AR protein through its AR antagonist portion ａnd von Hippel-Lindau (VHL)/cullin 2 E3 ligase through its VHL ligand portion to recruit AR protein to cullin 2 for ubiquitination, followed by proteasome-dependent AR degradation.
ARD-61 (0.001-100 μM; for 7 days) has IC₅₀ values of 235 nM ａnd 121 nM in the MDA-MB-453 ａnd HCC1428 cell lines, which have the highest AR expression, respectively. ARD-61 demonstrates partial cell growth inhibition, delivering IC₅₀ values of 39, 147, ａnd 380 nM, respectively, in the MCF-7, BT-549 ａnd MDA-MB-415 cell lines, which have a moderate level of AR protein.
ARD-61 (25-100000 nM; 6-72 h) induces G2/M cell cycle arrest in a dose- ａnd time-dependent manner in each of these three AR+ breast cancer cell lines.
ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 ａnd HCC1428 cell lines.
ARD-61 (0.01-1000 nM; 6 h) is highly potent ａnd effective in reducing AR protein levels. ARD-61 (0.01-1000 nM; 24 h) reduces the level of PR protein with a DC₅₀ value of 0.15 nM in the T47D cells. ARD-61 has no obvious effect on ER ａnd GR proteins.
ARD-61 (1 µM; for 24 h) effectively inhibits Wnt/β-catenin ａnd MYC signaling pathways. ARD-61 (1-1000 nM; for 24 h) not only decreases both phosphorylated HER2 ａnd HER3, but also un-phosphorylated HER2 ａnd HER3 proteins.
Efficient knock-down of VHL completely blocks AR degradation induced by ARD-61 (100 nM; 24 h) in both MDA-MB-453 ａnd MCF-7 cell lines.

In Vivo: ARD-61 (25, 50 mg/kg/day; ip; for 75 days) effectively inhibits tumor growthin the MDA-MB-453 xenograft tumor model in male SCID mice.
ARD-61 (25 mg/kg; ip; single dose) effectively ａnd rapidly reduces the AR protein in the MDA-MB-453 xenograft tissue, with the effect persisting for at least 24 h. ARD-61 is very effective in reducing the mRNA level of WNT7B in a time-dependent manner.

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