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Foretinib

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产品编号 T3113Cas号 849217-64-7
别名 XL880, GSK1363089, GSK089, EXEL-2880

Foretinib (GSK1363089) 是多靶点酪氨酸激酶抑制剂,能够抑制 Met (IC50:0.4 nM) 和 KDR (IC50:0.9 nM)。

Foretinib

Foretinib

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纯度: 99.7%
产品编号 T3113 别名 XL880, GSK1363089, GSK089, EXEL-2880Cas号 849217-64-7

Foretinib (GSK1363089) 是多靶点酪氨酸激酶抑制剂,能够抑制 Met (IC50:0.4 nM) 和 KDR (IC50:0.9 nM)。

规格价格库存数量
1 mg¥ 342现货
2 mg¥ 488现货
5 mg¥ 822现货
10 mg¥ 1,370现货
25 mg¥ 2,330现货
50 mg¥ 3,490现货
100 mg¥ 4,960现货
500 mg¥ 10,600现货
1 mL x 10 mM (in DMSO)¥ 996现货
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产品介绍

生物活性
产品描述
Foretinib (GSK1363089) is a broad-spectrum tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
靶点活性
FLT4:2.8 nM (cell free), FLT3:3.6 nM (cell free), RON:3 nM (cell free), KDR:0.86 nM (cell free), Tie2:1.1 nM (cell free), MET:0.4 nM (cell free)
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]。
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].
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].
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].
别名XL880, GSK1363089, GSK089, EXEL-2880
化学信息
分子量632.65
分子式C34H34F2N4O6
CAS No.849217-64-7
SmilesCOc1cc2c(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3F)ccnc2cc1OCCCN1CCOCC1
密度1.372g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 63.3 mg/mL (100 mM)
DMSO: 40 mg/mL (63.23 mM)
溶液配制表
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.5807 mL7.9033 mL15.8065 mL79.0326 mL
5 mM0.3161 mL1.5807 mL3.1613 mL15.8065 mL
10 mM0.1581 mL0.7903 mL1.5807 mL7.9033 mL
20 mM0.0790 mL0.3952 mL0.7903 mL3.9516 mL
50 mM0.0316 mL0.1581 mL0.3161 mL1.5807 mL
Ethanol
1mg5mg10mg50mg
100 mM0.0158 mL0.0790 mL0.1581 mL0.7903 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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