化合物 Foretinib|T3113

價(jià)格	￥342	￥488	￥822
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-14

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產(chǎn)品詳情

中文名稱:化合物 Foretinib	英文名稱:Foretinib
CAS:849217-64-7	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.7%	產(chǎn)品類別: 抑制劑
貨號(hào): T3113

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實(shí)驗(yàn)	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].
激酶實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	Foretinib (EXEL-2880) 針對(duì)HGF受體家族的酪氨酸激酶展現(xiàn)抑制作用，其IC50值對(duì)于Met為0.4 nmol/L，對(duì)于Ron為3 nmol/L。EXEL-2880同樣抑制KDR, Flt-1和Flt-4，IC50值分別為0.9, 6.8和2.8 nmol/L。EXEL-2880是對(duì)細(xì)胞內(nèi)Met的強(qiáng)效抑制劑，在PC-3前列腺細(xì)胞和小鼠B16F10黑色素瘤細(xì)胞中的IC50值分別為23和21 nmol/L [1]。在MKN-45中，1 μM foretinib能夠抑制MET的磷酸化和下游信號(hào)分子。此外，1 μM foretinib也能抑制FGFR2和下游分子的磷酸化，說明foretinib針對(duì)KATO-III中的FGFR2。Foretinib通過抑制MET，在MKN-45中抑制表皮生長因子受體(EGFR)、HER3和FGFR3的磷酸化，并通過抑制FGFR2在KATO-III中抑制EGFR、HER3和MET的磷酸化 [2]。
體內(nèi)活性	通過單次口服灌胃給藥，100 mg/kg的EXEL-2880可顯著抑制B16F10腫瘤Met的磷酸化，效果持續(xù)到24小時(shí)。EXEL-2880的每日一次口服灌胃給藥，呈劑量依賴性減少腫瘤負(fù)擔(dān)，分別在30和100 mg/kg的劑量下減少了31%和62%。EXEL-2880處理后，肺表面腫瘤負(fù)擔(dān)（通過每個(gè)腫瘤的總結(jié)節(jié)數(shù)乘以平均結(jié)節(jié)直徑計(jì)算）分別在30和100 mg/kg劑量下減少了50%和58% [1]。Foretinib的每日口服給藥（30 mg/kg）顯著抑制了所有三種腫瘤異種移植物的生長，從給藥后僅七天開始，并持續(xù)整個(gè)實(shí)驗(yàn)過程。此外，經(jīng)過14天Foretinib治療后，所有標(biāo)本中的TEN細(xì)胞腫瘤異種移植物完全消失[3]。
存儲(chǔ)條件	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)
關(guān)鍵字	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
相關(guān)產(chǎn)品	Ribociclib \| Axitinib \| Sorafenib tosylate \| Lenvatinib mesylate \| Sanguinarine chloride \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| L-Ascorbic acid 2-phosphate trisodium \| Regorafenib monohydrate \| Nintedanib esylate
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 已知活性化合物庫 \| 激酶抑制劑庫 \| 膜蛋白靶向化合物庫 \| 酪氨酸激酶分子庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字： GSK089|||EXEL-2880|||GSK1363089|||XL880|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號(hào)4樓

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