| Description | Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively) |
| In vitro | IPI-549使多柔比星耐药的SW620/Ad300细胞对P-糖蛋白(P-gp)底物敏感，例如紫杉醇（紫杉醇单独使用与联合IPI-549使用的IC50分别为710和6.7 nM），并提高了SW620/Ad300细胞内紫杉醇的水平[1]。 |
| In vivo | IPI-549 在体内展现出有益的药代动力学属性，并且对 PI3K-γ 介导的中性粒细胞迁移具有强效抑制作用[2]。 |
| Animal experiments | SW620 (4 X 10^6 ) and SW620/Ad300 (5 X 10^6 ) cells were injected subcutaneously at the flank near the armpits of athymic nude mice.?When the subcutaneous tumors were approximately 0.5 x 0.5 cm in size (day 0), the mice were randomized into four treatment groups.?The vehicle used to deliver the IPI-549 and paclitaxel by intraperitoneal (i.p.) injection was ethanol/Cremophor ELP/saline (10%/10%/80%).?Group one received the vehicle only;?group two received vehicle plus 3 mg/kg IPI-549;?group three received vehicle plus 15 mg/kg paclitaxel;?group four, the combination group, received vehicle plus 3 mg/kg IPI-549 one h prior to administration of vehicle plus 15 mg/kg paclitaxel.?The drug doses were administered every 3 days with a total of 4 doses.?Tumor volume was measured using calipers, and body weights were recorded prior to each dosing. |
| Target activity | PI3Kγ:16 nM |
| Synonyms | IPI-549 |
| molecular weight | 528.56 |
| Molecular formula | C30H24N8O2 |
| CAS | 1693758-51-8 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 1 mg/ml, Sonication is recommended. |
| References | 1. De Vera AA1, Gupta P.et al.Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo.Cancer Lett. 2019 Feb 1;442:91-103 2. Evans CA, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. |
| Citations | 1. Jiang Y, Xiong W, Jia L, et al. Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations. European Journal of Medicinal Chemistry. 2022: 114824. 2. Xiong W, Jia L, Liang J, et al. Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study. International Immunopharmacology. 2022, 111: 109102 3. Xiong W, Jia L, Liang J, et al.Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study.International Immunopharmacology.2022, 111: 109102. 4. 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. |