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.
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- Pureté: 99.69%
- CAS No.: 915087-27-3
- Formule: C22H16F4N4O2S
- Masse moléculaire:476.45
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Nuclear Receptor Compound Library
HY-L126
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Anti-Drug-Resistant Compound Library
HY-L169
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Cancer Compound Library
HY-L025
Activité biologique
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Cell Line
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Type | Value | Description | References |
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| 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] |
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.
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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.
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.
Chemical Information
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CAS No. 915087-27-3
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Appearance Solid
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Masse moléculaire 476.45
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 Related Classifications
HY-111145 Related Classifications
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