| Description | IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant/immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases. |
| In vitro | IPN60090对GLS1具有小于100nM(IC50)的抑制活性，并且对A549细胞增殖具有小于100纳摩尔(EC50)的半最大有效浓度。[1] |
| In vivo | IPN-60090 (100 mg/kg; 口服; 每日两次; 连续30天;) 显著抑制肿瘤生长，并且在剂量依赖性方式中展现出强有力的体内靶向作用。IPN-60090在给药后4小时，第4天和第28天的谷氨酸/谷氨酰胺比例以及血浆中的游离浓度均有所降低。[2]IPN60090（3 mg/kg; 静脉注射; 经口给药为10 mg/kg）具有优良的药代动力学属性，清除率(CL)为4.1 mL/min/kg，半衰期(t1/2)为1小时，最大浓度(Cmax)为19 μM，生物利用度(F%)为89%。[2] |
| Target activity | GLS1:31 nM (IC50) |
| Synonyms | GLS1-IN-1 |
| molecular weight | 532.52 |
| Molecular formula | C24H27F3N8O3 |
| CAS | 1853164-83-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (51.64 mM), Sonication is recommended. |
| References | 1. Maria Emilia Di Francesco, et al. Gls1 inhibitors for treating disease. WO2016004404A2. 2. Soth MJ, et al. Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties. J Med Chem. 2020;63(21):12957-12977. 3. Wang D, et al. An updated patent review of glutaminase inhibitors (2019-2022). Expert Opin Ther Pat. 2023;33(1):17-28. |
| Citations | 1. Gong K, Huang Y, Zheng Y, et al.ZSWIM4 inhibition improves chemosensitivity in epithelial ovarian cancer cells by suppressing intracellular glycine biosynthesis.Journal of Translational Medicine.2024, 22(1): 1-21. |