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- 2025年12月05日
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- 文献和实验
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Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
- CAS号：
2316837-08-6
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1 mg///5 mg
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ARD-61
CAS No. : 2316837-08-6
MCE 国际站：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 | Vitamin D Related/Nuclear Receptor | 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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文献和实验27 4.24 3.65 3.31 3.08 2.92 2.80 2.71 2.63 2.57 2.47 2.36 2.25 2.13 2.00 1.85 27 28 4.22 3.63 3.29 3.06 2.90 2.78 2.69 2.61 2.55 2.45 2.34 2.23 2.11 1.98 1.83 28 29 4.20 3.61 3.27 3.04 2.88 2.76 2.67 2.59 2.53 2.43 2.32 2.21 2.09 1.96 1.81 29
08 11 12 44 95 92 63 16 29 56 24 29 48 39 26 99 61 65 53 58 37 78 80 70 42 10 50 67 42 32 17 55 85 74 94 44 67 16 94 40 14 65 52 68 75 87 59 36 22 41 26 78 63 06 55 13 08 27 01 50 15 29 39 39 43 41 17 53 77 58 71 71 41 61 50 72 12 41 94 96 26 44 95
去抄两个数。分别以8，7除之，余数即指要调入乙组的第几个甲，余此类推。最后各组的鼠数就相等了。调整后各组鼠的编号为： 组别鼠的编号 甲组3 4 5 7 8 12 乙组1 2 6 9 10 11 （二）当分为三组时 例：设有雄性的SD大鼠12只，按体重大小依次编为1，2，3，…，12号，试用完全随机的方法，分为A、B、C三组。 分组方法：假设所定的点是随机数字表第40行17列的08，则从08开始，自左到右抄12个随机
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