ARD-266
Based on 1 Customer Validation
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM. ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(Pink: Target protein ligand; Blue: VHL E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2666951-70-6
- Formula: C52H59ClN6O7
- Molecular Weight:915.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | DC50 |
0.5352 nM
Compound: 11; ARD-266
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Protac activity against VHL/AR in AR-positive human LNCAP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis
Protac activity against VHL/AR in AR-positive human LNCAP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis
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[PMID: 31804827] |
| LNCaP | IC50 |
2 nM
Compound: 11; ARD-266
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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
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[PMID: 31804827] |
| VCaP | DC50 |
0.9686 nM
Compound: 11; ARD-266
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Protac activity against VHL/AR in AR-positive human VCaP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis
Protac activity against VHL/AR in AR-positive human VCaP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis
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[PMID: 31804827] |
| VCaP | IC50 |
6 nM
Compound: 11; ARD-266
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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
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[PMID: 31804827] |
ARD-266 (Compound 11; 100 nM; 1-24 hours; LNCaP and VCaP cells) treatment effectively reduces the AR protein level within 3 h and achieves near-complete AR elimination with a 6 h treatment in the LNCaP cells[1].
ARD-266 (Compound 11; 1-10000 nM; 24 hours; LNCaP cells) treatment effectively suppresses the expression of PSA, TMPRSS2, and FKBP5 genes in a dosedependent manner and is capable of reducing the mRNA levels of PSA, TMPRSS2, and FKBP5 genes by >50% at 10 nM in the LNCaP cell line[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:100 nM
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Incubation Time:1 hour, 3 hours, 6 hours, 12 hours, 24 hours
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Result:Effectively reduced the AR protein level within 3 h and achieved near-complete AR elimination with a 6 h treatment in the LNCaP cells.
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Cell Line:LNCaP cells
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Concentration:1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:24 hours
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Result:Effectively suppressed the expression of PSA, TMPRSS2, and FKBP5 genes in a dose-dependent manner and was capable of reducing the mRNA levels of PSA, TMPRSS2, and FKBP5 genes by >50% at 10 nM in the LNCaP cell line.
Chemical Information
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CAS No. 2666951-70-6
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Appearance Solid
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Molecular Weight 915.51
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Formula C52H59ClN6O7
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Color White to off-white
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SMILES
O=C(C[C@@H](C1=CC=CC=C1)NC([C@H]2N(C([C@H](C(C)C)C3=CC(C)=NO3)=O)C[C@H](O)C2)=O)N(CC4)CCC4C#CC5=CC=C(C(N[C@@H]6C(C)(C)[C@@H](OC7=CC=C(C#N)C(Cl)=C7)C6(C)C)=O)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (109.23 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (5.46 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (5.46 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0923 mL | 5.4614 mL | 10.9229 mL | 27.3072 mL |
| 5 mM | 0.2185 mL | 1.0923 mL | 2.1846 mL | 5.4614 mL | |
| 10 mM | 0.1092 mL | 0.5461 mL | 1.0923 mL | 2.7307 mL | |
| 15 mM | 0.0728 mL | 0.3641 mL | 0.7282 mL | 1.8205 mL | |
| 20 mM | 0.0546 mL | 0.2731 mL | 0.5461 mL | 1.3654 mL | |
| 25 mM | 0.0437 mL | 0.2185 mL | 0.4369 mL | 1.0923 mL | |
| 30 mM | 0.0364 mL | 0.1820 mL | 0.3641 mL | 0.9102 mL | |
| 40 mM | 0.0273 mL | 0.1365 mL | 0.2731 mL | 0.6827 mL | |
| 50 mM | 0.0218 mL | 0.1092 mL | 0.2185 mL | 0.5461 mL | |
| 60 mM | 0.0182 mL | 0.0910 mL | 0.1820 mL | 0.4551 mL | |
| 80 mM | 0.0137 mL | 0.0683 mL | 0.1365 mL | 0.3413 mL | |
| 100 mM | 0.0109 mL | 0.0546 mL | 0.1092 mL | 0.2731 mL |
ARD-266 Related Classifications
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