2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  3. PROTACs Androgen Receptor Progesterone Receptor Apoptosis
  4. ARD-61

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。

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ARD-61 Chemical Structure

ARD-61 Chemical Structure

CAS No. : 2316837-08-6

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ARD-61 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1]. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

VHL

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
LNCaP IC50
2 nM
Compound: 1; ARD-61
Antiproliferative activity against AR-positive human LNCAP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
Antiproliferative activity against AR-positive human LNCAP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
[PMID: 31804827]
VCaP IC50
2 nM
Compound: 1; ARD-61
Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
[PMID: 31804827]
体外研究
(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[1].
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[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 DC50 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].

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

ARD-61 相关抗体:

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 (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[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].

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[1]
Dosage: 25, 50 mg/kg
Administration: IP; daily; for 75 days
Result: Effectively inhibited tumor growth.
分子量

1095.78

Formula

C61H71ClN8O7S
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (91.26 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    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); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.68%

COA (284 KB) HNMR (177 KB) RP-HPLC (268 KB)

产品使用指南 (1538 KB)
参考文献

ARD-61 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9126 mL 4.5630 mL 9.1259 mL 22.8148 mL
5 mM 0.1825 mL 0.9126 mL 1.8252 mL 4.5630 mL
10 mM 0.0913 mL 0.4563 mL 0.9126 mL 2.2815 mL
15 mM 0.0608 mL 0.3042 mL 0.6084 mL 1.5210 mL
20 mM 0.0456 mL 0.2281 mL 0.4563 mL 1.1407 mL
25 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9126 mL
30 mM 0.0304 mL 0.1521 mL 0.3042 mL 0.7605 mL
40 mM 0.0228 mL 0.1141 mL 0.2281 mL 0.5704 mL
50 mM 0.0183 mL 0.0913 mL 0.1825 mL 0.4563 mL
60 mM 0.0152 mL 0.0760 mL 0.1521 mL 0.3802 mL
80 mM 0.0114 mL 0.0570 mL 0.1141 mL 0.2852 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARD-612316837-08-6ARD61ARD 61PROTACsAndrogen ReceptorProgesterone ReceptorApoptosisNR3C3MDA-MB-453cullinE3ligaseHCC1428MCF-7BT-549MDA-MB-415Inhibitorinhibitorinhibit

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