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).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.57%
- CAS. Nr.: 2632305-17-8
- Formel: C43H45ClN8O5
- Molecular Weight:789.32
-
Speicherung:
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]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ARD-2051
MoreAlle PROTACs Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
IC50 & Target
|
Cereblon |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
13 nM
Compound: 30; ARD-2051
|
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
|
[PMID: 37382562] |
| VCaP | IC50 |
10 nM
Compound: 30; ARD-2051
|
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
|
[PMID: 37382562] |
In Vitro
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.
-
Cell Line:LNCaP and VCaP cells
-
Concentration:0.03, 0.1, 0.3, 1, 3, 10, 30 nM
-
Incubation Time:24 h
-
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 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:VCaP cells (5 × 106 in 5 mg/mL Matrigel) were subcutaneously implanted into the flanks of male CB17 SCID mice[1]
-
Dosage:3.5, 7.5, 12.5, 25 mg/kg
-
Administration:p.o. daily for 21 days
-
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.
Chemical Information
-
CAS. Nr. 2632305-17-8
-
Appearance Solid
-
Molecular Weight 789.32
-
Formel C43H45ClN8O5
-
Color Light yellow to yellow
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Anal Chem
Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]2025 Dec 2;97(47):26097-26107. PMID: 41243541
Lösungsmittel & Löslichkeit
In Vitro:
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (271 KB)
-
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)
-
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 (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 Related Classifications
HY-149862 Related Classifications
Powered by Bioz