| Description | Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others. |
| In vitro | Pilaralisib 在小儿临床前测试计划 (PPTP) 细胞系展示出细胞毒活性，中位相对IC50值为10.9 mM（范围从2.7 mM到24.5 mM）。[2] |
| In vivo | 在 BALB/c nu/nu 小鼠中，Pilaralisib（100 mg/kg，p.o.）能有效抑制实体胶质瘤异种移植物的生长。Pilaralisib 的耐受性良好，治疗组的毒性率仅为0.7%。[2] 在无胸腺雌性小鼠中，Pilaralisib（100 mg/kg，p.o.）显著延缓肿瘤生长，且未观察到显著的药物相关毒性。[3] |
| Cell experiments | Cell proliferation is measured by using MTT or pre-mixed WST-1 reagent. For MTT/WST-1 assays, 10,000 cells/well are seeded in 96-well plates. 24 h after plating, cells are treated with DMSO or pilaralisib. After 5 days of treatment, MTT/WST-1 assays are performed.(Only for Reference) |
| Target activity | PI3Kγ:23 nM, PI3Kα:39 nM, PI3Kβ:36 nM, PI3Kδ:36 nM |
| Synonyms | SAR245408, XL-147 |
| molecular weight | 541.02 |
| Molecular formula | C25H25ClN6O4S |
| CAS | 934526-89-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (171.9 mM) |
| References | 1. Foster P, et al. Mol Cancer Ther. 2015, 14(4), 931-940. 2. Reynolds CP, et al. Pediatr Blood Cancer. 2013, 60(5), 791-798. 3. Chakrabarty A, et al. Proc Natl Acad Sci U S A. 2012, 109(8), 2718-2723. 4. Yu P, et al. Mol Cancer Ther. 2014, 13(5), 1078-1091. 5. Rexer BN, et al. Clin Cancer Res. 2013, 19(19), 5390-5401. |