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Foretinib

产品编号 T3113 CAS 849217-64-7

别名: GSK089, EXEL-2880, GSK1363089, XL880

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)。

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Foretinib, CAS 849217-64-7

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 996	现货

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其他形式的 Foretinib:

Foretinib phosphate
询价

选择批次

纯度: 99.7%

纯度: 98.07%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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), Tie2:1.1 nM (cell free), KDR:0.86 nM (cell free), MET:0.4 nM (cell free)
体外活性	Foretinib (EXEL-2880) inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nmol/L for Met and 3 nmol/L for Ron. EXEL-2880 also inhibits KDR, Flt-1, and Flt-4 with IC50 values of 0.9, 6.8, and 2.8 nmol/L, respectively. EXEL-2880 is a potent inhibitor of cellular Met with IC50 values of 23 and 21 nmol/L, respectively, in PC-3 prostate cells and murine B16F10 melanoma cells [1]. In MKN-45, 1 μM of foretinib inhibited phosphorylation of MET and downstream signaling molecules. Further, 1 μM of foretinib inhibited phosphorylation of FGFR2 and downstream molecules, suggesting that foretinib targets FGFR2 in KATO-III. Foretinib inhibits phosphorylation of epidermal growth factor receptor (EGFR), HER3 and FGFR3 via MET inhibition in MKN-45, and EGFR, HER3 and MET via FGFR2 inhibition in KATO-III [2].
体内活性	A single 100 mg/kg oral gavage dose of EXEL-2880 resulted in substantial inhibition of phosphorylation of B16F10 tumor Met, which persisted through 24 h. Once daily oral gavage administration of EXEL-2880 resulted in a dose-dependent reduction in tumor burden of 31% and 62%, respectively, for doses of 30 and 100 mg/kg. The lung surface tumor burden, calculated by multiplying the total nodule count by the average nodule diameter for each tumor, was reduced by 50% and 58% following treatment with 30 and 100 mg/kg EXEL-2880, respectively [1]. The daily oral administration of foretinib (30 mg/kg) significantly inhibited the growth of tumor in all three of the tumor xenografts starting after only seven days of administration, and lasting throughout the experiment. Moreover, TEN cell tumor xenografts completely vanished in all specimens after 14 days of foretinib treatment [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	GSK089, EXEL-2880, GSK1363089, XL880
分子量	632.65
分子式	C34H34F2N4O6
CAS No.	849217-64-7

存储

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

溶解度

Ethanol: 63.3 mg/mL (100 mM)

DMSO: 63.3 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.5807 mL	7.9033 mL	15.8065 mL	39.5163 mL
	5 mM	0.3161 mL	1.5807 mL	3.1613 mL	7.9033 mL
	10 mM	0.1581 mL	0.7903 mL	1.5807 mL	3.9516 mL
	20 mM	0.079 mL	0.3952 mL	0.7903 mL	1.9758 mL
	50 mM	0.0316 mL	0.1581 mL	0.3161 mL	0.7903 mL
	100 mM	0.0158 mL	0.079 mL	0.1581 mL	0.3952 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Qian F, et al. Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res, 2009, 69(20), 8009-8016. 2. Kataoka Y, et al. Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs, 2011. 3. Kogata Y, et al. Foretinib (GSK1363089) induces p53-dependent apoptosis in endometrial cancer. Oncotarget. 2018 Apr 27;9(32):22769-22784.

文献引用

1. Wang P, Zhang Y, Xiang R, et al.Foretinib is effective in acute myeloid leukemia by inhibiting FLT3 and overcoming secondary mutations that drive resistance to quizartinib and gilteritinib.Cancer Research.2024

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Foretinib 849217-64-7 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Tie-2 c-Met/HGFR GSK-1363089 inhibit GSK-089 GSK089 XL-880 GSK 1363089 Inhibitor EXEL-2880 GSK 089 GSK1363089 EXEL 2880 XL880 Vascular endothelial growth factor receptor EXEL2880 XL 880 inhibitor

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Foretinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

Keywords