化合物 Foretinib|T3113

Foretinib
849217-64-7

￥342 1mg 起订

￥488 2mg 起订

￥822 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Foretinib

英文名称：: Foretinib

CAS号：: 849217-64-7

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.7%

产品类别：: 抑制剂

货号：: T3113

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.
溶解度	Ethanol : 63.3 mg/mL (100 mM) DMSO : 40 mg/mL (63.23 mM)
关键字	c-Met/HGFR \| GSK-1363089 \| inhibit \| GSK-089 \| XL-880 \| GSK 1363089 \| Inhibitor \| GSK 089 \| VEGFR \| Foretinib \| EXEL 2880 \| Vascular endothelial growth factor receptor \| EXEL2880 \| XL 880
相关产品	Ribociclib \| Axitinib \| Sorafenib tosylate \| Lenvatinib mesylate \| Sanguinarine chloride \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| L-Ascorbic acid 2-phosphate trisodium \| Regorafenib monohydrate \| Taxifolin
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

XL880|||GSK1363089|||GSK089|||EXEL-2880|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子