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  • 化合物 Glumetinib|T5414|TargetMol

化合物 Glumetinib|T5414|TargetMol

Glumetinib
1642581-63-2
￥413 1mg 起订
￥987 5mg 起订
￥1650 10mg 起订
上海 更新日期：2025-02-28

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 Glumetinib
英文名称：
Glumetinib
CAS号：
1642581-63-2
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：
100%
产品类别：
抑制剂
货号：
T5414

Product Introduction

Bioactivity

名称Glumetinib
描述Glumetinib (SCC244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).
细胞实验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.
激酶实验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.
动物实验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%.
体外活性Glumetinib在使用ELISA激酶测定法对纯化的c-Met激酶活性表现出高效能(IC50: 0.42 nM)。Glumetinib对c-Met的选择性超过了2,400倍，远高于所评估的312种激酶，包括c-Met家族成员RON以及与之高度同源的激酶Axl、Mer和TyrO3。Glumetinib强烈抑制了HGF诱导的NCI-H441细胞的迁移和侵袭能力，并且在10 nmol/L的剂量下足以阻止大多数细胞的移动，显示出剂量依赖性的作用。
体内活性在MKN-45模型中，Glumetinib以10、5和2.5 mg/kg的剂量分别显著抑制肿瘤生长，抑制率分别为99.3%、88.6%和63.6%。此外，在使用5和10 mg/kg剂量的Glumetinib进行21天治疗后，观察到肿瘤停滞。在SNU-5模型中使用Glumetinib治疗得到了类似结果，并且在高剂量组中观察到肿瘤回归。在EBC-1研究中，所有接受Glumetinib治疗的小鼠，其肿瘤质量均减少了超过66.0%，且在10和5 mg/kg治疗组中，每6只小鼠中就有1只未发现肿瘤。此外，在所有测试模型中，Glumetinib在10 mg/kg的效力与INCB28060在15 mg/kg和crizotinib在50 mg/kg的效力相当。
存储条件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.
关键字Glumetinib | proliferation | tumor | cancer | bioavailable | oral | HCC | inhibit | c-Met/HGFR | SCC-244 | ATP-competitive | cell | NSCLC | Inhibitor | SCC 244
相关产品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
相关库抑制剂库 | 抗癌活性化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 高选择性抑制剂库 | 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
SCC244|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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