ARD-61|cas:2316837-08-6|西域试剂

ARD-61,99.68%

产品编号：Bellancom-139659| CAS NO：2316837-08-6| 分子式：C₆₁H₇₁ClN₈O₇S| 分子量：1095.78

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-139659		￥9000.00	杭州北京（现货）

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ARD-61

产品介绍

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。

生物活性

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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

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 (DC₅₀=0.44 nM), MCF-7 (DC₅₀=1.8 nM), BT549 (DC₅₀=2.0 nM), MDA-MB-415 (DC₅₀=2.4 nM) and HCC1428 (DC₅₀=3.0 nM) cell lines.

体内研究
(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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (91.26 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9126 mL	4.5630 mL	9.1259 mL
5 mM	0.1825 mL	0.9126 mL	1.8252 mL
10 mM	0.0913 mL	0.4563 mL	0.9126 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (2.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (2.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。