| Description | Nemiralisib（GSK-2269557 free base） is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease. |
| In vitro | Nemiralisib 在周围血液单个核细胞 (PBMC) 中抑制 IFNγ (pIC50: 9.7)。Nemiralisib 对 PI3Kδ 具有高度选择性，与密切相关的同型体 PI3Kα (pIC50: 5.3)、PI3Kβ (pIC50: 5.8) 和 PI3Kγ (pIC50: 5.2) 相比，选择性>1000倍。[1] |
| In vivo | Nemiralisib在与II型助T细胞(Th2)驱动的肺部炎症相关的病症模型中表现出活性，该模型为布朗挪威大鼠急性OVA模型。通过对斯普莱格道利雄性大鼠的药代动力学数据的获取，评估了该系列化合物以吸入方式给药的适应性，包括在大鼠微粒体中的清除数据，随后在体内进行评估。Nemiralisib 通过口服或静脉注射给药，剂量分别为3和1mg/kg（每种给药方式2只大鼠）。[1] |
| Target activity | PI3Kγ:5.2 (pic50), PI3Kα:5.3 (pic50), PI3Kβ:5.8 (pic50), PI3Kδ:9.9 (pki) |
| Synonyms | GSK2269557 (free base), GSK2269557 |
| molecular weight | 440.54 |
| Molecular formula | C26H28N6O |
| CAS | 1254036-71-9 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 29 mg/mL (65.83 mM), Sonication is recommended. |
| References | 1. Down K et al. Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. J Med Chem. 2015 Sep 24;58(18):7381-99. |