ARD-61 T39853

Product Introduction
Bioactivity


英文名: ARD-61

描述: ARD-61 is a potent and specific PROTAC androgen receptor (AR) degrader, exhibiting high effectiveness. It effectively induces the degradation of AR and progesterone receptors (PR) in AR+ cancer cell lines, leading to apoptosis. Additionally, ARD-61 demonstrates significant tumor growth inhibition in the MDA-MB-453 xenograft model in mice.

体外活性: 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[1]. ARD-61 (0.001-100 μM; for 7?days) has IC 50 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 IC 50 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[1]. 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[1]. ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 and HCC1428 cell lines[1]. 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 DC 50 value of 0.15?nM in the T47D cells. ARD-61 has no obvious effect on ER and GR proteins[1]. 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[1]. 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[1]. Cell Viability Assay[1]Cell Line: MDA-MB-453 and HCC1428 cell lines Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Time: 7?days Result: Achieves near complete inhibition of cell growth. Cell Cycle Analysis[1]Cell Line: MDA-MB-453, HCC1428 and MCF-7 cell lines Concentration: 25, 250, 500, 1000, 10000, 100000 nM Incubation Time: 6-72 hours Result: Induced G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines. Apoptosis Analysis[1]Cell Line: MDA-MB-453 and HCC1428 cell lines Concentration: 25, 250, 500, 1000, 10000, 100000 nM Incubation Time: 6-72 hours Result: Induced apoptosis in the MDA-MB-453 and HCC1428 cell lines in a dose-dependent manner. Western Blot Analysis[1]Cell Line: MDA-MB-453, MCF-7, BT549, MDA-MB-415 and HCC1428 cell lines Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation Time: 6 hours Result: Reduced AR protein levels in the MDA-MB-453 (DC 50 =0.44?nM), MCF-7 (DC 50 =1.8?nM), BT549 (DC 50 =2.0?nM), MDA-MB-415 (DC 50 =2.4?nM) and HCC1428 (DC 50 =3.0?nM) cell lines.

体内活性: 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[1]. 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[1]. Animal Model: MDA-MB-453 xenograft tumor model in male SCID mice[1]Dosage: 25, 50?mg/kg Administration: IP; daily; for 75 days Result: Effectively inhibited tumor growth.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: ARD-61 | ARD 61 | ARD61

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途