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.
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: 99.88%
- CAS 番号: 2215022-45-8
- 分子式: C27H29N5O4S2
- 分子量:551.68
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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
生物活性
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PI3Kγ |
PI3Kδ 9.2 μM (IC50) |
PI3Kα 7.2 μM (IC50) |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2215022-45-8
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性状 Solid
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分子量 551.68
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分子式 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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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
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |