计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice
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 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. 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 DC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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 AnalysisCell 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 AnalysisCell 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.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MDA-MB-453 xenograft tumor model in male SCID mice Dosage: 25, 50 mg/kg Administration: IP; daily; for 75 days Result: Effectively inhibited tumor growth.
Form:Solid
IC50& Target:VHL
规格
规格或纯度
≥99%
英文名称
ARD-61
生化机理
ARD-61 是一种强效、有效和特异的 PROTAC 雄激素受体（AR）降解剂。ARD-61 能有效诱导 AR+ 癌细胞系中的 AR 和孕酮受体（PR）降解。ARD-61 可诱导细胞凋亡，并有效诱导肿瘤细胞凋亡。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
1095.78
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (91.26 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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