ARD-2051
Based on 1 publication(s) in Google Scholar
ARD-2051 is a selective and orally active androgen receptor (AR) PROTAC degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer.
(Pink: Androgen Receptor ligand (HY-400666); Blue: Cereblon ligand (HY-14658); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.57%
- CAS 番号: 2632305-17-8
- 分子式: C43H45ClN8O5
- 分子量:789.32
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 ARD-2051
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生物活性
製品説明
IC50 & Target
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Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
13 nM
Compound: 30; ARD-2051
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Growth inhibition in human LNCaP cells incubated for 4 days by WST-8 assay
Growth inhibition in human LNCaP cells incubated for 4 days by WST-8 assay
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[PMID: 37382562] |
| VCaP | IC50 |
10 nM
Compound: 30; ARD-2051
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Growth inhibition in human VCaP cells incubated for 4 days by WST-8 assay
Growth inhibition in human VCaP cells incubated for 4 days by WST-8 assay
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[PMID: 37382562] |
体外実験
ARD-2051 (0.6 nM, 24 h) induces AR protein degradation in LNCaP and VCaP cells with a DC50 of 0.6 nM and Dmax of 92% and 97%, respectively[1].
ARD-2051 (10-13 nM, 4 days) inhibits cell growth in LNCaP and VCaP cells with an IC50 of 12.8 nM and 10.2 nM respectively[1].
ARD-2051 (0.03-30 nM, 24 h) dose-dependently suppresses the expression of AR-regulated gene KLK3 in LNCaP and VCaP cells[1].
ARD-2051 (0.01-1 μM, 24 h) selectively degrades AR protein in VCaP cells, with no significant effect on over 5,700 other proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP and VCaP cells
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Concentration:0.03, 0.1, 0.3, 1, 3, 10, 30 nM
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Incubation Time:24 h
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Result:Suppressed the expression of AR-regulated gene KLK3 in LNCaP and VCaP cells.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-t | CL | Vss | Cmax | F |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 1 mg/kg | i.v. | 8.9 h | 3.235 mg·h/L | 4.6 mL/min/kg | 2.8 L/kg | / | / |
| Dog[1] | 3 mg/kg | p.o. | 3.4 h | 4.464 mg·h/L | / | / | 294 mg/mL | 46 % |
| Mice[1] | 2 mg/kg | i.v. | 5 h | 8.846 mg·h/L | 3.7 mL/min/kg | 1.3 L/kg | / | / |
| Mice[1] | 5 mg/kg | p.o. | 4.9 h | 11.684 mg·h/L | / | / | 1476 mg/mL | 53 % |
| Rat[1] | 1 mg/kg | i.v. | 2.1 h | 1.563 mg·h/L | 10.2 mL/min/kg | 1.3 L/kg | / | / |
| Rat[1] | 10 mg/kg | p.o. | 3.9 h | 12.781 mg·h/L | / | / | 1473 mg/mL | 82 % |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:VCaP cells (5 × 106 in 5 mg/mL Matrigel) were subcutaneously implanted into the flanks of male CB17 SCID mice[1]
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Dosage:3.5, 7.5, 12.5, 25 mg/kg
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Administration:p.o. daily for 21 days
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Result:Achieved tumor growth inhibition (TGI) rates of 44%, 71%, 61%, and 80% at doses of 3.75, 7.5, 12.5, and 25 mg/kg.
Showed no significant changes in body weight.
化学情報
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CAS 番号 2632305-17-8
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性状 Solid
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分子量 789.32
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分子式 C43H45ClN8O5
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Color Light yellow to yellow
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SMILES
O=C(C1=C2C=CC(N3CC(N4CCN(C(C5=CC=C(C=C5)N6CCC7(CC6)CN([C@H](C7)C)C8=CC(Cl)=C(C=C8)C#N)=O)CC4)C3)=C1)N(C2=O)C9C(NC(CC9)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Anal Chem
Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]2025 Dec 2;97(47):26097-26107. PMID: 41243541
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (31.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2669 mL | 6.3346 mL | 12.6691 mL | 31.6728 mL |
| 5 mM | 0.2534 mL | 1.2669 mL | 2.5338 mL | 6.3346 mL | |
| 10 mM | 0.1267 mL | 0.6335 mL | 1.2669 mL | 3.1673 mL | |
| 15 mM | 0.0845 mL | 0.4223 mL | 0.8446 mL | 2.1115 mL | |
| 20 mM | 0.0633 mL | 0.3167 mL | 0.6335 mL | 1.5836 mL | |
| 25 mM | 0.0507 mL | 0.2534 mL | 0.5068 mL | 1.2669 mL | |
| 30 mM | 0.0422 mL | 0.2112 mL | 0.4223 mL | 1.0558 mL |
ARD-2051 関連分類
HY-149862 関連分類
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