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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.58%
- CAS 番号: 2484757-20-0
- 分子式: C19H15D4ClN6O2
- 分子量:402.87
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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.
化学情報
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CAS 番号 2484757-20-0
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非標識Cas 1297538-32-9
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性状 Solid
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分子量 402.87
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分子式 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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別名
ODM-201-d4; BAY-1841788-d4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-16985S 関連分類
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- 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