GS-9901
Based on 1 Customer Validation
GS-9901 is a highly selective and orally active PI3Kδ inhibitor with an IC50 of 1 nM. GS-9901 has ≥100 fold selectivity for PI3Kα (IC50 of 750 nM), PI3Kβ (IC50 of 100 nM) and PI3Kγ (IC50 of 190 nM). GS-9901 can be used for the study of rheumatoid arthritis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.97%
- No. CAS: 1640247-87-5
- Fòrmula: C22H17ClFN9O
- Peso molecular:477.88
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Almacenamiento:Powder -20°C, 3 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
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PI3Kδ 1 nM (IC50) |
PI3Kβ 100 nM (IC50) |
PI3Kγ 190 nM (IC50) |
PI3Kα 750 nM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats with established collagen-induced arthritis (CIA)[1].
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Dosage:0.3 mg/kg, 1 mg/kg, and 3 mg/kg.
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Administration:Orally, twice-daily for 7 days starting on the 10th day after the second collagen immunization.
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Result:Demonstrated significant reduction in ankle swelling in rats treated with 0.3 mg/kg 35 (31% reduction), 1 mg/kg 35 (67%), and 3 mg/kg 35 (65%).
Plasma concentrations measured on day 7 (12 h after last dose) were consistent with maintaining approximately 60%, 80%, and >90% inhibition of PI3Kδ at 0.3, 1.0, and 3 mg/kg doses, respectively, at trough levels.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1640247-87-5
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Appearance Solid
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Peso molecular 477.88
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Fòrmula C22H17ClFN9O
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Color White to off-white
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SMILES
NC1=NC(N)=NC(N[C@H](C2CC2)C(N3C4=CN=CC=C4)=NC5=C(F)C=CC(Cl)=C5C3=O)=C1C#N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : ≥ 250 mg/mL (523.14 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 2.0926 mL | 10.4629 mL | 20.9258 mL | 52.3144 mL |
| 5 mM | 0.4185 mL | 2.0926 mL | 4.1852 mL | 10.4629 mL | |
| 10 mM | 0.2093 mL | 1.0463 mL | 2.0926 mL | 5.2314 mL | |
| 15 mM | 0.1395 mL | 0.6975 mL | 1.3951 mL | 3.4876 mL | |
| 20 mM | 0.1046 mL | 0.5231 mL | 1.0463 mL | 2.6157 mL | |
| 25 mM | 0.0837 mL | 0.4185 mL | 0.8370 mL | 2.0926 mL | |
| 30 mM | 0.0698 mL | 0.3488 mL | 0.6975 mL | 1.7438 mL | |
| 40 mM | 0.0523 mL | 0.2616 mL | 0.5231 mL | 1.3079 mL | |
| 50 mM | 0.0419 mL | 0.2093 mL | 0.4185 mL | 1.0463 mL | |
| 60 mM | 0.0349 mL | 0.1744 mL | 0.3488 mL | 0.8719 mL | |
| 80 mM | 0.0262 mL | 0.1308 mL | 0.2616 mL | 0.6539 mL | |
| 100 mM | 0.0209 mL | 0.1046 mL | 0.2093 mL | 0.5231 mL |
GS-9901 Related Classifications
HY-100694 Related Classifications
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