AZD8154
Based on 1 Customer Validation
AZD8154 is a selective PI3Kγδ dual inhibitor. AZD8154 can suppress PI3Kγ and PI3Kδ signaling pathway activation. AZD8154 can be used for the researches of inflammation and immunology, such as asthma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- No. CAS: 2215022-45-8
- Fòrmula: C27H29N5O4S2
- Peso molecular:551.68
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[3]|
PI3Kγ |
PI3Kδ 9.2 μM (IC50) |
PI3Kα 7.2 μM (IC50) |
In Vitro
AZD8154 (0.1-1000 nM) inhibits CD11b and CD86 expression in rat splenic B cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats models of OVA (HY-W250978)-induced allergic asthma[1]
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Dosage:0.02, 0.1 and 0.3 mg/kg
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Administration:Intratracheally administration, on day 28 1h prior to OVA challenge
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Result:Suppressed pAkt levels in the lung tissuse.
Decreased neutrophils and eosinophils.
Decreased late asthmatic response.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2215022-45-8
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Appearance Solid
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Peso molecular 551.68
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Fòrmula C27H29N5O4S2
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Color Light yellow to yellow
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SMILES
CS(=O)(C1=C2C(CN(C2=O)[C@H](C3CC3)C)=CC(C4=C(C)N=C(NC5=CC=CC(N6C(CCC6)=O)=N5)S4)=C1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (45.32 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)
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pinkerton JW, et al. PI3Kγδ inhibition suppresses key disease features in a rat model of asthma. Respir Res. 2024 Apr 23;25(1):175. [Content Brief]
[2]. Sadiq MW, et al. Characterisation of pharmacokinetics, safety and tolerability in a first-in-human study for AZD8154, a novel inhaled selective PI3Kγδ dual inhibitor targeting airway inflammatory disease. Br J Clin Pharmacol. 2022 Jan;88(1):260-270. [Content Brief]
[3]. Perry MWD, et al. Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma. J Med Chem. 2021 Jun 24;64(12):8053-8075. [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 | 1.8126 mL | 9.0632 mL | 18.1265 mL | 45.3161 mL |
| 5 mM | 0.3625 mL | 1.8126 mL | 3.6253 mL | 9.0632 mL | |
| 10 mM | 0.1813 mL | 0.9063 mL | 1.8126 mL | 4.5316 mL | |
| 15 mM | 0.1208 mL | 0.6042 mL | 1.2084 mL | 3.0211 mL | |
| 20 mM | 0.0906 mL | 0.4532 mL | 0.9063 mL | 2.2658 mL | |
| 25 mM | 0.0725 mL | 0.3625 mL | 0.7251 mL | 1.8126 mL | |
| 30 mM | 0.0604 mL | 0.3021 mL | 0.6042 mL | 1.5105 mL | |
| 40 mM | 0.0453 mL | 0.2266 mL | 0.4532 mL | 1.1329 mL |
AZD8154 Related Classifications
HY-115870 Related Classifications
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