| Description | Duvelisib (INK1197) is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. |
| In vitro | 在小鼠和大鼠中,用IPI-145(10 mg/kg)处理,表现出良好的动力学效应.在大鼠CIA模型中,IPI-145 能够防止发炎,并且保护关节骨和软骨. |
| In vivo | IPI-145能够抑制多种淋巴细胞增殖,在鼠 B细胞(EC50=0.5 nM),人类 B细胞(EC50=0.5 nM),人类T细胞(EC50=9.5 nM)。 |
| Target activity | PI3Kβ:1564 pM(Ki), PI3Kδ:23 pM(Ki), PI3Kγ:243 pM(Ki) |
| Synonyms | INK1197, IPI-145, 度维利塞 |
| molecular weight | 416.86 |
| Molecular formula | C22H17ClN6O |
| CAS | 1201438-56-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 1 mg/ml, Sonication is recommended. |
| References | 1. Vito Palombella, Targeting PI3K- δ and PI3K-γ in Inflammation, 2012. |
| Citations | 1. Xiong W, Jia L, Cai Y, et al.Evaluation of the anti-inflammatory effects of PI3Kδ/γ inhibitors for treating acute lung injury.Immunobiology.2023: 152753. 2. Sugawara T, Nevedomskaya E, Heller S, et al.Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis.Molecular Oncology.2024 |