购物车
  • 全部删除
  • TargetMol
    您的购物车当前为空

Glumetinib

Rating icon 很棒
产品编号 T5414Cas号 1642581-63-2
别名 SCC244

Glumetinib (SCC244) 是一种高选择性、ATP 竞争性的、口服具有活力的 c-Met 抑制剂。它对 c-Met 的选择性超过 312 种激酶,包括 c-Met 家族成员 RON 和高度同源的激酶 Axl、Mer、TyrO3。它具有抗肿瘤作用。

Glumetinib
TargetMol

为众多的药物研发团队赋能,

让新药发现更简单!

Glumetinib

Rating icon 很棒
纯度: 100%
产品编号 T5414 别名 SCC244Cas号 1642581-63-2

Glumetinib (SCC244) 是一种高选择性、ATP 竞争性的、口服具有活力的 c-Met 抑制剂。它对 c-Met 的选择性超过 312 种激酶,包括 c-Met 家族成员 RON 和高度同源的激酶 Axl、Mer、TyrO3。它具有抗肿瘤作用。

规格价格库存数量
1 mg¥ 413现货
5 mg¥ 987现货
10 mg¥ 1,650现货
25 mg¥ 2,780现货
50 mg¥ 3,930现货
100 mg¥ 5,720现货
大包装 & 定制
加入购物车
实验操作小课堂
查看更多

"Glumetinib"的相关化合物库

选择批次:
纯度:100%
联系我们获取更多批次信息
TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。

产品介绍

生物活性
产品描述
Glumetinib (SCC244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).
靶点活性
c-Met:0.42 nM (cell free)
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。
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.
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.
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%.
别名SCC244
化学信息
分子量459.48
分子式C21H17N9O2S
CAS No.1642581-63-2
SmilesCn1cc(cn1)-c1cnc2cnn(c2c1)S(=O)(=O)c1cnc2ccc(cn12)-c1cnn(C)c1
密度1.61 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 4.59 mg/mL (10 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.1764 mL10.8819 mL21.7637 mL108.8187 mL
5 mM0.4353 mL2.1764 mL4.3527 mL21.7637 mL
10 mM0.2176 mL1.0882 mL2.1764 mL10.8819 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

关键词

评论列表

4个月前
5.0
Rating icon 很棒

评论内容

Related Tags: buy Glumetinib | purchase Glumetinib | Glumetinib cost | order Glumetinib | Glumetinib chemical structure | Glumetinib in vivo | Glumetinib in vitro | Glumetinib formula | Glumetinib molecular weight