ARD-2128
Based on 1 Customer Validation
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
(Pink: Androgen Receptor ligand (HY-172624); Blue: Cereblon ligand (HY-W087383); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 2222111-87-5
- Formula: C45H50ClN7O6
- Molecular Weight:820.37
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Storage:
-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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 4 nM (VCaP), 5 μM (LNCaP)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
5 nM
Compound: 28; ARD-2128
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Growth inhibition of human LNCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay
Growth inhibition of human LNCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay
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[PMID: 34431670] |
| VCaP | IC50 |
4 nM
Compound: 28; ARD-2128
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Growth inhibition of human VCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay
Growth inhibition of human VCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay
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[PMID: 34431670] |
ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values of 4 nM and 5 nM, respectively[1].
ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VCaP cell
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Concentration:1, 10, 100, and 1000 nM
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Incubation Time:24 hours
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Result:Reduces the AR protein level and achieves the AR degradation.
ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice[1].
ARD-2128 (5mg/kg; p.o.) treatment shows the Cmax, AUC0-t and t1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice[1]
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Dosage:20 mg/kg
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Administration:Oral
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Result:Reducing the level of AR protein in mice after 24 hours.
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Animal Model:SCID mice[1]
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Dosage:10, 20, and 40 mg/kg
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Administration:P.o.; daily for 21 days
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Result:Inhibits tumor growth by 46, 69, and 63%, respectively.
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Animal Model:Male ICR Mice[1]
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Dosage:5 mg/kg
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Administration:P.o. (Pharmacokinetic Analysis)
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Result:The Cmax, AUC0-t and t1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
Chemical Information
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CAS No. 2222111-87-5
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Appearance Solid
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Molecular Weight 820.37
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Formula C45H50ClN7O6
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Color Light yellow to green yellow
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SMILES
O=C(N[C@H]1C(C)(C)[C@H](OC2=CC=C(C#N)C(Cl)=C2)C1(C)C)C3=CC=C(N4CCN(CC5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)CC5)CC4)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-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)
Solvent & Solubility
DMSO : 100 mg/mL (121.90 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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)
- Portuguese - PT (252 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, 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 | 1.2190 mL | 6.0948 mL | 12.1896 mL | 30.4741 mL |
| 5 mM | 0.2438 mL | 1.2190 mL | 2.4379 mL | 6.0948 mL | |
| 10 mM | 0.1219 mL | 0.6095 mL | 1.2190 mL | 3.0474 mL | |
| 15 mM | 0.0813 mL | 0.4063 mL | 0.8126 mL | 2.0316 mL | |
| 20 mM | 0.0609 mL | 0.3047 mL | 0.6095 mL | 1.5237 mL | |
| 25 mM | 0.0488 mL | 0.2438 mL | 0.4876 mL | 1.2190 mL | |
| 30 mM | 0.0406 mL | 0.2032 mL | 0.4063 mL | 1.0158 mL | |
| 40 mM | 0.0305 mL | 0.1524 mL | 0.3047 mL | 0.7619 mL | |
| 50 mM | 0.0244 mL | 0.1219 mL | 0.2438 mL | 0.6095 mL | |
| 60 mM | 0.0203 mL | 0.1016 mL | 0.2032 mL | 0.5079 mL | |
| 80 mM | 0.0152 mL | 0.0762 mL | 0.1524 mL | 0.3809 mL | |
| 100 mM | 0.0122 mL | 0.0609 mL | 0.1219 mL | 0.3047 mL |
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