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- CAS号:
1693758-51-8
- 规格:
1mg/2mg/5mg/10mg/25mg/50mg/100mg/500mg
| 规格: | 1mg | 产品价格: | ¥225.0 |
|---|---|---|---|
| 规格: | 2mg | 产品价格: | ¥306.0 |
| 规格: | 5mg | 产品价格: | ¥463.0 |
| 规格: | 10mg | 产品价格: | ¥713.0 |
| 规格: | 25mg | 产品价格: | ¥1456.0 |
| 规格: | 50mg | 产品价格: | ¥2136.0 |
| 规格: | 100mg | 产品价格: | ¥3176.0 |
| 规格: | 500mg | 产品价格: | ¥6944.0 |
Product Introduction
Bioactivity
| 名称 | Eganelisib |
| 描述 | Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively) |
| 动物实验 | SW620 (4 X 10^6 ) and SW620/Ad300 (5 X 10^6 ) cells were injected subcutaneously at the flank near the armpits of athymic nude mice.?When the subcutaneous tumors were approximately 0.5 x 0.5 cm in size (day 0), the mice were randomized into four treatment groups.?The vehicle used to deliver the IPI-549 and paclitaxel by intraperitoneal (i.p.) injection was ethanol/Cremophor ELP/saline (10%/10%/80%).?Group one received the vehicle only;?group two received vehicle plus 3 mg/kg IPI-549;?group three received vehicle plus 15 mg/kg paclitaxel;?group four, the combination group, received vehicle plus 3 mg/kg IPI-549 one h prior to administration of vehicle plus 15 mg/kg paclitaxel.?The drug doses were administered every 3 days with a total of 4 doses.?Tumor volume was measured using calipers, and body weights were recorded prior to each dosing. |
| 体外活性 | IPI-549使多柔比星耐药的SW620/Ad300细胞对P-糖蛋白(P-gp)底物敏感,例如紫杉醇(紫杉醇单独使用与联合IPI-549使用的IC50分别为710和6.7 nM),并提高了SW620/Ad300细胞内紫杉醇的水平[1]。 |
| 体内活性 | IPI-549 在体内展现出有益的药代动力学属性,并且对 PI3K-γ 介导的中性粒细胞迁移具有强效抑制作用[2]。 |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 20 mg/mL (37.84 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.17 mg/mL (7.89 mM), Solution. 10% DMSO+90% Saline : < 2.61 mg/mL (4.94 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. |
| 关键字 | PI3Kγ | PI3Kβ | PI3Kα | PI3K | Phosphoinositide 3-kinase | IPI549 | IPI 549 | Inhibitor | inhibit | Eganelisib |
| 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 | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Fibrosis Compound Library | Anti-Aging Compound Library | Highly Selective Inhibitor Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical 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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