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- CAS号:
934526-89-3
- 规格:
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/500mg
| 规格: | 1mg | 产品价格: | ¥228.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥591.0 |
| 规格: | 2mg | 产品价格: | ¥318.0 |
| 规格: | 5mg | 产品价格: | ¥495.0 |
| 规格: | 10mg | 产品价格: | ¥794.0 |
| 规格: | 25mg | 产品价格: | ¥1336.0 |
| 规格: | 50mg | 产品价格: | ¥1984.0 |
| 规格: | 100mg | 产品价格: | ¥3184.0 |
| 规格: | 500mg | 产品价格: | ¥6768.0 |
Product Introduction
Bioactivity
| 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 : 6.25 mg/mL (11.55 mM), Solution. 10% DMSO+90% Saline : < 6.25 mg/mL (11.55 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 62.5 mg/mL (115.52 mM), Sonication is recommended. |
| 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 | Musk ketone | Quercetin | Hyaluronic acid | Berberine sulfate | Methyl eugenol | Myricetin | Quercitrin hydrate | Isoprenaline hydrochloride | 4-Vinylcyclohexene Dioxide |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Kinase Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | PI3K-AKT-mTOR Compound Library | Anti-Cancer Drug Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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