化合物Pilaralisib T2365

Product Introduction
Bioactivity


英文名: Pilaralisib

描述: Pilaralisib (XL-147) 是一种有效的、选择性的 I 类PI3Ks 抑制剂，能够抑制 PI3Kα (IC50:39 nM)，PI3Kβ (IC50:383 nM)，PI3Kγ (IC50:23 nM) 和 PI3Kδ (IC50:36 nM)。

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: In BALB/c nu/nu mice, Pilaralisib (100 mg/kg, p.o.) induces tumor growth inhibition for solid glioma xenografts. Pilaralisib is well tolerated, with only 0.7% toxicity rate in the treated groups, similar to that observed for control animals.[2] In athymic female mouse, Pilaralisib (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (171.9 mM)


关键字: Pilaralisib | inhibit | PI3K | XL147 | Phosphoinositide 3-kinase | Inhibitor | SAR-245408 | SAR 245408 | XL 147

相关产品: Pilaralisib analogue | ETP-45658 | GSK2292767 | PI3Kα-IN-14 | Bakkenolide A | PI3K/mTOR Inhibitor-2 | Sonolisib | PI3Kδ-IN-12 | CHMFL-PI3KD-317 | TG100-115

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Autophagy Compound Library | Reprogramming Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途