化合物 Glumetinib|T5414|TargetMol

價(jià)格	￥413	￥987	￥1650
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 Glumetinib	英文名稱:Glumetinib
CAS:1642581-63-2	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 100%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T5414

Product Introduction

Bioactivity

名稱	Glumetinib
描述	Glumetinib (SCC244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).
細(xì)胞實(shí)驗(yàn)	Cells were seeded in 96-well plates at a low density in growth media. The next day, appropriate controls or designated concentrations of compounds were added to each well, and the cells were incubated for 72 hours. HUVECs (passage 3) were seeded in 96-well plates in growth media overnight and transferred to serum-free media for 24 hours. The following day, appropriate controls or designated concentrations of compounds were added to each well, and HGF was added to designated wells at 100 ng/mL. The cells were incubated for 48 hours. Finally, cell proliferation was determined using a sulforhodamine B assay, a thiazolyl blue tetrazolium bromide assay or a cell counting kit (CCK-8) assay.
激酶實(shí)驗(yàn)	Met, Ron, Axl, TyrO3, and Mer kinases activity were assessed using both ELISA and radiometric protein kinase assays. The kinase selectivity profile of SCC244 (1 μmol/L) was screened against a panel of other 308 recombinant kinases using radiometric protein kinase assays was also performed according to the manufacturer's specifications.
動(dòng)物實(shí)驗(yàn)	To assess the pharmacodynamics of SCC244 in tumors, mice bearing established xenograft tumors were treated with a single dose of the compound at 10 or 2.5 mg/kg, and tumors were harvested at several time points. At a designated time following administration, mice were humanely euthanized, and their tumors were resected. The tumors were snap-frozen in liquid nitrogen and then homogenized in 500 μL of protein extraction solution (radioimmunoprecipitation assay, RIPA). The tumor extracts were then subjected to Western blot analysis. The individual bands of phospho-c-Met, phospho-AKT, and phospho-ERK were scanned and quantified using Gel Pro Analyzer software. The relative tyrosine phosphorylation of each sample at the indicated time points was then calculated, with the average value of vehicle-treated sample used as 100%.
體外活性	Glumetinib在使用ELISA激酶測(cè)定法對(duì)純化的c-Met激酶活性表現(xiàn)出高效能(IC50: 0.42 nM)。Glumetinib對(duì)c-Met的選擇性超過(guò)了2,400倍，遠(yuǎn)高于所評(píng)估的312種激酶，包括c-Met家族成員RON以及與之高度同源的激酶Axl、Mer和TyrO3。Glumetinib強(qiáng)烈抑制了HGF誘導(dǎo)的NCI-H441細(xì)胞的遷移和侵襲能力，并且在10 nmol/L的劑量下足以阻止大多數(shù)細(xì)胞的移動(dòng)，顯示出劑量依賴性的作用。
體內(nèi)活性	在MKN-45模型中，Glumetinib以10、5和2.5 mg/kg的劑量分別顯著抑制腫瘤生長(zhǎng)，抑制率分別為99.3%、88.6%和63.6%。此外，在使用5和10 mg/kg劑量的Glumetinib進(jìn)行21天治療后，觀察到腫瘤停滯。在SNU-5模型中使用Glumetinib治療得到了類(lèi)似結(jié)果，并且在高劑量組中觀察到腫瘤回歸。在EBC-1研究中，所有接受Glumetinib治療的小鼠，其腫瘤質(zhì)量均減少了超過(guò)66.0%，且在10和5 mg/kg治療組中，每6只小鼠中就有1只未發(fā)現(xiàn)腫瘤。此外，在所有測(cè)試模型中，Glumetinib在10 mg/kg的效力與INCB28060在15 mg/kg和crizotinib在50 mg/kg的效力相當(dāng)。
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	DMSO : 4.59 mg/mL (10 mM), Sonication is recommended.
關(guān)鍵字	Glumetinib \| proliferation \| tumor \| cancer \| bioavailable \| oral \| HCC \| inhibit \| c-Met/HGFR \| SCC-244 \| ATP-competitive \| cell \| NSCLC \| Inhibitor \| SCC 244
相關(guān)產(chǎn)品	Capmatinib 2HCl \| Cabozantinib S-malate \| Crizotinib \| Amuvatinib \| BMS 777607 \| (±)-Norcantharidin \| Capmatinib xHCl \| LMTK3-IN-1 \| L-Ascorbic acid 2-phosphate trisodium \| Norcantharidin \| Bacitracin Zinc \| AMG-458
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 高選擇性抑制劑庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： SCC244|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專(zhuān)業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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