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- CAS号：
849217-64-7
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥289.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥796.0 |
| 规格： | 5mg | 产品价格： | ￥654.0 |
| 规格： | 10mg | 产品价格： | ￥944.0 |
| 规格： | 25mg | 产品价格： | ￥1832.0 |
| 规格： | 50mg | 产品价格： | ￥2776.0 |
| 规格： | 100mg | 产品价格： | ￥3944.0 |
Product Introduction
Bioactivity
| 名称 | Foretinib |
| 描述 | Foretinib (GSK1363089) is a broad-spectrum tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR. |
| 细胞实验 | PC-3 and B16F10 cells were seeded in 24-well plates overnight. The cells were then washed and incubated with serum-free medium for 3 h followed by a 1 h incubation with EXEL-2880 before addition of HGF (100 ng/mL) for 10 min. Met phosphorylation status was determined by ELISA analysis (Supplementary Data). For determination of VEGF-stimulated extracellular signal-regulated kinase phosphorylation, human umbilical vein endothelial cells were seeded in 96-well plates and incubated for 24 h and then serum-starved for another 24 h. A serial dilution of EXEL-2880 was added for 1 h before a 5 min stimulation with VEGF (20 ng/mL). Medium was removed, and the cells were fixed with Cytofix and then treated with 0.6% H2O2. Plates were blocked with 10% FBS and incubated with a mouse monoclonal anti-phosphorylated extracellular signal-regulated kinase p44/42 antibody (E10) followed by incubation with goat anti-mouse IgG-horseradish peroxidase and chemiluminescent detection. IC50 values were calculated based on triplicate experiments [1]. |
| 激酶实验 | Kinase inhibition was investigated using one of three assay formats: [33P]phosphoryl transfer, luciferase-coupled chemiluminescence, or AlphaScreen tyrosine kinase technology. Further assay details are provided in Supplementary Section. IC50 values were calculated by nonlinear regression analysis using XLFit [1]. |
| 动物实验 | B16F10 tumor cells (2 × 10^5) were implanted via i.v. tail vein injection into mice on day 0. EXEL-2880 or vehicle administration was initiated 3 days after implantation for 10 days followed by assessment of lung tumor burden. Lungs were excised, weighed, and zinc-fixed for 24 h, and the number of nodules formed on all lobe surfaces was counted using a Zeiss stereoscope. Lung nodule diameters were morphometrically measured on digitally captured images. Inhibition of tumor burden as measured by lung wet weight was calculated as follows: % tumor growth inhibition = [(compound treated-naive / vehicle-naive) × 100]. The results for each treatment group (n = 10 animals) were averaged, and statistical t test analysis was done comparing each treatment group to the vehicle-treated control [1]. |
| 体外活性 | Foretinib (EXEL-2880) 针对HGF受体家族的酪氨酸激酶展现抑制作用，其IC50值对于Met为0.4 nmol/L，对于Ron为3 nmol/L。EXEL-2880同样抑制KDR, Flt-1和Flt-4，IC50值分别为0.9, 6.8和2.8 nmol/L。EXEL-2880是对细胞内Met的强效抑制剂，在PC-3前列腺细胞和小鼠B16F10黑色素瘤细胞中的IC50值分别为23和21 nmol/L [1]。在MKN-45中，1 μM foretinib能够抑制MET的磷酸化和下游信号分子。此外，1 μM foretinib也能抑制FGFR2和下游分子的磷酸化，说明foretinib针对KATO-III中的FGFR2。Foretinib通过抑制MET，在MKN-45中抑制表皮生长因子受体(EGFR)、HER3和FGFR3的磷酸化，并通过抑制FGFR2在KATO-III中抑制EGFR、HER3和MET的磷酸化 [2]。 |
| 体内活性 | 通过单次口服灌胃给药，100 mg/kg的EXEL-2880可显著抑制B16F10肿瘤Met的磷酸化，效果持续到24小时。EXEL-2880的每日一次口服灌胃给药，呈剂量依赖性减少肿瘤负担，分别在30和100 mg/kg的剂量下减少了31%和62%。EXEL-2880处理后，肺表面肿瘤负担（通过每个肿瘤的总结节数乘以平均结节直径计算）分别在30和100 mg/kg剂量下减少了50%和58% [1]。Foretinib的每日口服给药（30 mg/kg）显著抑制了所有三种肿瘤异种移植物的生长，从给药后仅七天开始，并持续整个实验过程。此外，经过14天Foretinib治疗后，所有标本中的TEN细胞肿瘤异种移植物完全消失[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 : 63.3 mg/mL (100.06 mM), Sonication is recommended. DMSO : 40 mg/mL (63.23 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.16 mM), Sonication is recommended. |
| 关键字 | XL-880 | XL 880 | VEGFR3/FLT4 | VEGFR2 (KDR) | VEGFR | Vascular endothelial growth factor receptor | Tie-2 | Tie2 | RON | Met | Inhibitor | inhibit | HGFR | GSK-1363089 | GSK-089 | GSK 1363089 | GSK 089 | Foretinib | EXEL2880 | EXEL 2880 | c-Met/HGFR | cMet/HGFR | c-Met | cMet |
| 相关产品 | glycine | Ribociclib | Lenvatinib | Afatinib | Chloramphenicol | Thymoquinone | Regorafenib | Pazopanib | Sorafenib | Decanoic Acid | Nintedanib esylate | Bacitracin Zinc |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | Kinase Inhibitor Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library | Reprogramming Compound Library |
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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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化合物 Foretinib【849217-64-7】
￥289 - 3944
