ARD-61
Based on 1 Customer Validation
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. 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.57%
- No. CAS: 2316837-08-6
- Fòrmula: C61H71ClN8O7S
- Peso molecular:1095.78
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | DC50 |
7.2 nM
Compound: 1; ARD-61
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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: 1; ARD-61
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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 |
1 nM
Compound: 1; ARD-61
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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 |
2 nM
Compound: 1; ARD-61
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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
|
[PMID: 31804827] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-453 and HCC1428 cell lines
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Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:7 days
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Result:Achieves near complete inhibition of cell growth.
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Cell Line:MDA-MB-453, HCC1428 and MCF-7 cell lines
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Concentration:25, 250, 500, 1000, 10000, 100000 nM
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Incubation Time:6-72 hours
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Result:Induced G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines.
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Cell Line:MDA-MB-453 and HCC1428 cell lines
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Concentration:25, 250, 500, 1000, 10000, 100000 nM
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Incubation Time:6-72 hours
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Result:Induced apoptosis in the MDA-MB-453 and HCC1428 cell lines in a dose-dependent manner.
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Cell Line:MDA-MB-453, MCF-7, BT549, MDA-MB-415 and HCC1428 cell lines
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
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Incubation Time:6 hours
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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.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-453 xenograft tumor model in male SCID mice[1]
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Dosage:25, 50 mg/kg
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Administration:IP; daily; for 75 days
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Result:Effectively inhibited tumor growth.
Chemical Information
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No. CAS 2316837-08-6
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Appearance Solid
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Peso molecular 1095.78
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Fòrmula C61H71ClN8O7S
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Color White to light yellow
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SMILES
CC(C)([C@H](C1(C)C)NC(C2=CC=C(C=C2)C#CC3CCN(C4CCN(CC4)C(C[C@@H](C5=CC=C(C6=C(C)N=CS6)C=C5)NC([C@H]7N(C[C@@H](C7)O)C([C@@H](C8=CC(C)=NO8)C(C)C)=O)=O)=O)CC3)=O)[C@H]1OC9=CC(Cl)=C(C=C9)C#N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (91.26 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (2.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (2.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 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 |
ARD-61 Related Classifications
HY-139659 Related Classifications
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