RD162
Based on 1 Customer Validation
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human 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 : 98.97%
- CAS 番号: 915087-27-3
- 分子式: C22H16F4N4O2S
- 分子量:476.45
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
122 nM
Compound: 91
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Inhibition of prostate specific antigen expression in human LNCAP cells in presence of fetal bovine serum
Inhibition of prostate specific antigen expression in human LNCAP cells in presence of fetal bovine serum
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[PMID: 20218717] |
体外実験
RD162 (1-10 μM; 4 days) suppresses growth and induces apoptosis in the human prostate cancer cell line VCaP which has endogenous AR gene amplification[1].
RD162 has little to no binding to the progesterone, estrogen or glucocorticoid receptors in an in vitro fluorescence polarization assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:VCaP cells
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Concentration:1, 10 μM
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Incubation Time:4 days
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Result:Suppressed cell growth.
体内実験
RD162 (0.1, 1, 10 mg/kg; oral gavage; daily; for 5 days) consistently reduces luciferase activity with 10 mg/kg/day human LNCaP/AR xenografts grown in castrated male mice whereas lower doses of 0.1 and 1.0 mg/kg/day has minimal effect. RD162 substantially reduces cellular proliferation after 5 days[1].
RD162 (20 mg/kg; gavage) is ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Castrate male mice bearing LNCaP/AR xenografts[1]
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Dosage:10 mg/kg
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Administration:Oral gavage; daily; for 28 days
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Result:Caused all tumors regressed.
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Animal Model:Male mice[1]
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Dosage:20 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral gavage (in 0.5% hydroxy-methyl-propyl-cellulose)
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Result:Had ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours.
化学情報
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CAS 番号 915087-27-3
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性状 Solid
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分子量 476.45
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分子式 C22H16F4N4O2S
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Color White to off-white
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SMILES
O=C(NC)C1=CC=C(N(C(N(C2=CC=C(C#N)C(C(F)(F)F)=C2)C3=O)=S)C43CCC4)C=C1F
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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
体外:
DMSO : 125 mg/mL (262.36 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)
プロトコル
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
純度とドキュメンテーション
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データシート (280 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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取扱説明書 (2659 KB)
参考文献
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 | 2.0989 mL | 10.4943 mL | 20.9886 mL | 52.4714 mL |
| 5 mM | 0.4198 mL | 2.0989 mL | 4.1977 mL | 10.4943 mL | |
| 10 mM | 0.2099 mL | 1.0494 mL | 2.0989 mL | 5.2471 mL | |
| 15 mM | 0.1399 mL | 0.6996 mL | 1.3992 mL | 3.4981 mL | |
| 20 mM | 0.1049 mL | 0.5247 mL | 1.0494 mL | 2.6236 mL | |
| 25 mM | 0.0840 mL | 0.4198 mL | 0.8395 mL | 2.0989 mL | |
| 30 mM | 0.0700 mL | 0.3498 mL | 0.6996 mL | 1.7490 mL | |
| 40 mM | 0.0525 mL | 0.2624 mL | 0.5247 mL | 1.3118 mL | |
| 50 mM | 0.0420 mL | 0.2099 mL | 0.4198 mL | 1.0494 mL | |
| 60 mM | 0.0350 mL | 0.1749 mL | 0.3498 mL | 0.8745 mL | |
| 80 mM | 0.0262 mL | 0.1312 mL | 0.2624 mL | 0.6559 mL | |
| 100 mM | 0.0210 mL | 0.1049 mL | 0.2099 mL | 0.5247 mL |
RD162 関連分類
HY-111145 関連分類
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