Darolutamide-d4
Based on 1 Customer Validation
Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation. Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation. Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants. Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer.
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- Pureza : 98.58%
- No. CAS: 2484757-20-0
- Fòrmula: C19H15D4ClN6O2
- Peso molecular:402.87
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Aplicación
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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No. CAS 2484757-20-0
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Unlabeled CAS 1297538-32-9
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Appearance Solid
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Peso molecular 402.87
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Fòrmula C19H15D4ClN6O2
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Color White to off-white
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SMILES
O=C(C1=NNC(C([2H])(O)C([2H])([2H])[2H])=C1)N[C@@H](C)CN2N=C(C3=CC=C(C#N)C(Cl)=C3)C=C2
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Synonyms
ODM-201-d4; BAY-1841788-d4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (248.22 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)
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. [Content Brief]
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 | 2.4822 mL | 12.4110 mL | 24.8219 mL | 62.0548 mL |
| 5 mM | 0.4964 mL | 2.4822 mL | 4.9644 mL | 12.4110 mL | |
| 10 mM | 0.2482 mL | 1.2411 mL | 2.4822 mL | 6.2055 mL | |
| 15 mM | 0.1655 mL | 0.8274 mL | 1.6548 mL | 4.1370 mL | |
| 20 mM | 0.1241 mL | 0.6205 mL | 1.2411 mL | 3.1027 mL | |
| 25 mM | 0.0993 mL | 0.4964 mL | 0.9929 mL | 2.4822 mL | |
| 30 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0685 mL | |
| 40 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5514 mL | |
| 50 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.2411 mL | |
| 60 mM | 0.0414 mL | 0.2068 mL | 0.4137 mL | 1.0342 mL | |
| 80 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7757 mL | |
| 100 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6205 mL |
Darolutamide-d4 Related Classifications
HY-16985S Related Classifications
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Keywords
- Darolutamide-d4
- 2484757-20-0
- ODM-201-d4
- BAY-1841788-d4
- Isotope-Labeled Compounds
- Androgen Receptor
- androgen receptor (AR) competitive antagonist
- orally active
- inhibits AR nuclear translocation
- inhibits AR transcriptional activation
- selective for AR-positive cells
- full antagonist against AR mutants
- prostate cancer
- androgen receptor-dependent prostate cancer
- castration-resistant prostate cancer (CRPC)
- VCaP cells
- LNCaP cells (LN-AR-C cells)
- HS-HEK293 cells
- U2-OS cells
- DU-145 cells
- H1581 cells
- castrated male BALB/c nude mice
- intact athymic nude male mice
- male BalbC mice
- Balb/cOlaHsd mice
- Inhibitor
- inhibitor
- inhibit