| 名称 | Pilaralisib |
| 描述 | 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. |
| 细胞实验 | 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) |
| 激酶实验 | In vitro kinase inhibition assays: Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of the test compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.1 mM), Sonication is recommended.
DMSO : 93 mg/mL (171.9 mM), Sonication is recommended.
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| 关键字 | XL147 | XL 147 | SAR-245408 | SAR 245408 | Pilaralisib | PI3Kδ | PI3Kγ | PI3Kβ | PI3Kα | PI3K | Phosphoinositide 3-kinase | Inhibitor | inhibit |
| 相关产品 | 4-Methylbenzylidene camphor | Berberine hydrogen sulphate | Creatine monohydrate | (±)-α-Bisabolol | Heptadecanoic acid | Musk ketone | Quercetin | Hyaluronic acid | Berberine sulfate | Methyl eugenol | Myricetin | Isoprenaline hydrochloride |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 氧化还原化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 | 细胞重编程化合物库 |