2. Vitamin D Related/Nuclear Receptor PROTAC
  3. Androgen Receptor PROTACs
  4. ARD-69

ARD-69 是基于 E3 泛素连接酶 VHL、靶向雄激素受体的 PROTAC 降解剂，可诱导 AR 阳性前列腺癌细胞中雄激素受体 (AR) 蛋白降解。ARD-69 抑制 AR 调控的基因表达，一端结合 AR 配体结合域，另一端结合 VHL，促使 AR 招募至 E3 泛素连接酶复合体，触发蛋白酶体降解，从而抑制 AR 信号通路及下游基因 (如 PSA、TMPRSS2) 表达。ARD-69 可用于研究治疗去势抵抗性前列腺癌 (mCRPC) 的研究。

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ARD-69 Chemical Structure

ARD-69 Chemical Structure

CAS No. : 2316837-10-0

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1 mg ￥7500
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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-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC)[1][2][3].

IC50 & Target

Androgen receptor (AR)[1]
PROTAC[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CWR22R IC50
183 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay
Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay
[PMID: 30629437]
LNCaP IC50
0.25 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
[PMID: 30629437]
VCaP IC50
0.34 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
[PMID: 30629437]
体外研究
(In Vitro)

ARD-69 (0.01-10 μM；6-24 h) 呈剂量和时间依赖性诱导 LNCaP、VCaP 和 22Rv1 前列腺癌细胞的雄激素受体 (AR) 降解，DC50 分别为 0.86 nM、0.76 nM 和 10.4 nM，最高降解率 >95%[1]。
ARD-69 (0.01-1000 nM；7 d) 显著抑制 LNCaP、VCaP 和 22Rv1 细胞增殖，IC50 分别为 0.25 nM、0.34 nM 和 183 nM[1]。

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

Cell Viability Assay[1]

Cell Line: LNCaP, VCaP, 22Rv1 prostate cancer cells
Concentration: 0.01-1000 nM
Incubation Time: 7 days
Result: Inhibited cell growth with IC50s of 0.25 nM (LNCaP), 0.34 nM (VCaP), and 183 nM (22Rv1), significantly more effective (>100-fold) than AR antagonists like enzalutamide. qPCR analysis revealed dose-dependent suppression of AR-regulated genes (PSA, TMPRSS2, FKBP5) by >50% at 10 nM, while WB confirmed reduced AR protein levels correlating with growth inhibition.
体内研究
(In Vivo)

ARD-69 (50 mg/kg；腹腔注射；单次) 在严重联合免疫缺陷 (SCID) 小鼠的 VCaP 异种移植瘤模型中，显著降低肿瘤组织中的 AR 和 PSA 蛋白水平，效果持续至少 48 小时[1]。

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

Animal Model: Female severe combined immunodeficient (SCID) mice with VCaP xenograft tumors[1]
Dosage: 50 mg/kg, dissolved in an appropriate solvent (e.g., DMSO/saline formulation)
Administration: Intraperitoneal (IP) injection, single dose
Result: Significantly reduced androgen receptor (AR) and prostate-specific antigen (PSA) protein levels in tumor tissues, with effects detectable as early as 3 hours post-treatment and persisting for at least 48 hours.
Dose-dependently decreased in AR and PSA expression relative to the loading control GAPDH, indicating sustained pharmacodynamic activity in vivo.
分子量

1129.82

Formula

C62H74ClFN8O7S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 200 mg/mL (177.02 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8851 mL 4.4255 mL 8.8510 mL
5 mM 0.1770 mL 0.8851 mL 1.7702 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 (protect from light, stored under nitrogen)。-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

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动物溶解方案

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

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由于实验过程有损耗，建议您多配一只动物的量
纯度 & 产品资料
参考文献

ARD-69 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 (protect from light, stored under nitrogen)。-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 0.8851 mL 4.4255 mL 8.8510 mL 22.1274 mL
5 mM 0.1770 mL 0.8851 mL 1.7702 mL 4.4255 mL
10 mM 0.0885 mL 0.4425 mL 0.8851 mL 2.2127 mL
15 mM 0.0590 mL 0.2950 mL 0.5901 mL 1.4752 mL
20 mM 0.0443 mL 0.2213 mL 0.4425 mL 1.1064 mL
25 mM 0.0354 mL 0.1770 mL 0.3540 mL 0.8851 mL
30 mM 0.0295 mL 0.1475 mL 0.2950 mL 0.7376 mL
40 mM 0.0221 mL 0.1106 mL 0.2213 mL 0.5532 mL
50 mM 0.0177 mL 0.0885 mL 0.1770 mL 0.4425 mL
60 mM 0.0148 mL 0.0738 mL 0.1475 mL 0.3688 mL
80 mM 0.0111 mL 0.0553 mL 0.1106 mL 0.2766 mL
100 mM 0.0089 mL 0.0443 mL 0.0885 mL 0.2213 mL

Keywords:

ARD-692316837-10-0ARD69ARD 69Androgen ReceptorPROTACsAR-positive prostate cancer cell linesgene expressionInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-114402
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