| Description | AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects. |
| In vivo | AS-041164 (3-100 mg/kg p.o.) 通过剂量依赖性方式减少了小鼠RANTES诱导的中性粒细胞招募，其ED50值为27.35 mg/kg。AS-041164阻断了RANTES引发的趋化作用，并降低了AKT磷酸化水平。此外，AS-041164 (10-100 mg/kg；口服；一次性) 的治疗显著减轻了卡拉胶引起的爪子水肿炎症。 |
| Target activity | PI3Kδ:1.7 μM, PI3Kβ:1.4 μM, PI3Kα:240 nM, PI3Kγ:70 nM |
| molecular weight | 249.24 |
| Molecular formula | C11H7NO4S |
| CAS | 6318-41-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (501.52 mM), Sonication is recommended. |
| References | 1. Chiara Ferrandi, et al. Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. J Pharmacol Exp Ther. 2007 Sep;322(3):923-30. |