ORIC-101
Based on 1 Customer Validation
ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity. ORIC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.65%
- CAS. Nr.: 2222344-98-9
- Formel: C34H47NO2
- Molecular Weight:501.74
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
EC50: 5.6 nM (Glucocorticoid receptor)[1]
ORIC-101 shows markedly reduced androgen receptor agonism (EC50, 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC50, >10 μM)[1].
ORIC-101 (1-1000 nM) dose-dependently reduces the expression of n GR-mediated target gene (FKBP5 and GILZ), with IC50s of 17.2 and 21.2 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OVCAR5 xenograft tumor in cortisol-treated mice[1]
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Dosage:75 mg/kg with 100 mg/kg gemcitabine and 60 mg/kg carboplatin
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Administration:P.O. twice a day for 16-22 days
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Result:Significantly reduced tumor volume in combination with chemotherapeutic agents.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2222344-98-9
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Appearance Solid
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Molecular Weight 501.74
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Formel C34H47NO2
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Color White to off-white
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SMILES
CN(C(C)C)C1=CC=C([C@@H]2[C@@]([C@](CC3)([H])C(CC4)=CC3=O)([H])[C@]4([H])[C@@](CC[C@]5(C#CC(C)(C)C)O)([H])[C@]5(C)C2)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (199.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (275 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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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. 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 | 1.9931 mL | 9.9653 mL | 19.9306 mL | 49.8266 mL |
| 5 mM | 0.3986 mL | 1.9931 mL | 3.9861 mL | 9.9653 mL | |
| 10 mM | 0.1993 mL | 0.9965 mL | 1.9931 mL | 4.9827 mL | |
| 15 mM | 0.1329 mL | 0.6644 mL | 1.3287 mL | 3.3218 mL | |
| 20 mM | 0.0997 mL | 0.4983 mL | 0.9965 mL | 2.4913 mL | |
| 25 mM | 0.0797 mL | 0.3986 mL | 0.7972 mL | 1.9931 mL | |
| 30 mM | 0.0664 mL | 0.3322 mL | 0.6644 mL | 1.6609 mL | |
| 40 mM | 0.0498 mL | 0.2491 mL | 0.4983 mL | 1.2457 mL | |
| 50 mM | 0.0399 mL | 0.1993 mL | 0.3986 mL | 0.9965 mL | |
| 60 mM | 0.0332 mL | 0.1661 mL | 0.3322 mL | 0.8304 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2491 mL | 0.6228 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1993 mL | 0.4983 mL |