ARD-2585
Based on 1 Customer Validation
ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
(Pink: Androgen Receptor Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.19%
- CAS. Nr.: 2757422-79-8
- Formel: C41H43ClN8O5
- Molecular Weight:763.28
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Speicherung:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
16.2 nM
Compound: 43; ARD-2585
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Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability by WST-8 assay
Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability by WST-8 assay
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[PMID: 34473519] |
| LNCaP | IC50 |
16.2 nM
Compound: 141; ARD-2585
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Antiproliferative activity against human LNCaP cells
Antiproliferative activity against human LNCaP cells
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[PMID: 35786895] |
| VCaP | IC50 |
1.5 nM
Compound: 43; ARD-2585
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Growth inhibition of human VCaP cells assessed as cell viability by WST-8 assay
Growth inhibition of human VCaP cells assessed as cell viability by WST-8 assay
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[PMID: 34473519] |
| VCaP | IC50 |
1.5 nM
Compound: 141; ARD-2585
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Antiproliferative activity against human VCaP cells
Antiproliferative activity against human VCaP cells
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[PMID: 35786895] |
ARD-2585 achieves DC50 values of 0.04-0.1 nM in the VCaP cell line with AR gene amplification and in the LNCaP cell line carrying an AR mutation[1].
ARD-2585 (100 nM) is effective in reducing the AR protein level at the 3 and 24 h time-points by 78% (p < 0.01) and 60% at the 6 h time-point (p > 0.05)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2757422-79-8
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Appearance Solid
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Molecular Weight 763.28
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Formel C41H43ClN8O5
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Color Light yellow to green yellow
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SMILES
O=C(N(C1C(NC(CC1)=O)=O)C2=O)C(C2=C3)=CC=C3N(C4)CC4N(CC5)CCN5C(C=C6)=CC=C6C(N[C@@H]7CC[C@@H](N(C)C8=CC=C(C#N)C(Cl)=C8)CC7)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
DMSO : 85 mg/mL (111.36 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 4.25 mg/mL (5.57 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 4.25 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 (42.5 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: ≥ 4.25 mg/mL (5.57 mM); Clear solution
This protocol yields a clear solution of ≥ 4.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Reinheit & Dokumentation
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Data Sheet (269 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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Handling Instructions (2659 KB)
Verweise
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 (sealed storage, away from moisture and 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 | 1.3101 mL | 6.5507 mL | 13.1014 mL | 32.7534 mL |
| 5 mM | 0.2620 mL | 1.3101 mL | 2.6203 mL | 6.5507 mL | |
| 10 mM | 0.1310 mL | 0.6551 mL | 1.3101 mL | 3.2753 mL | |
| 15 mM | 0.0873 mL | 0.4367 mL | 0.8734 mL | 2.1836 mL | |
| 20 mM | 0.0655 mL | 0.3275 mL | 0.6551 mL | 1.6377 mL | |
| 25 mM | 0.0524 mL | 0.2620 mL | 0.5241 mL | 1.3101 mL | |
| 30 mM | 0.0437 mL | 0.2184 mL | 0.4367 mL | 1.0918 mL | |
| 40 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL | |
| 50 mM | 0.0262 mL | 0.1310 mL | 0.2620 mL | 0.6551 mL | |
| 60 mM | 0.0218 mL | 0.1092 mL | 0.2184 mL | 0.5459 mL | |
| 80 mM | 0.0164 mL | 0.0819 mL | 0.1638 mL | 0.4094 mL | |
| 100 mM | 0.0131 mL | 0.0655 mL | 0.1310 mL | 0.3275 mL |
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