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Glumetinib

产品编号 T5414 CAS 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。

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Glumetinib, CAS 1642581-63-2

规格	价格/CNY	货期
1 mg	￥ 483	现货
5 mg	￥ 1,120	现货
10 mg	￥ 1,730	现货
25 mg	￥ 2,930	现货
50 mg	￥ 4,380	现货
100 mg	￥ 6,230	现货
1 mL * 10 mM (in DMSO)	￥ 1,130	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Glumetinib (SCC244) (SCC 244) 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	SCC244 exhibited high potency (IC50: 0.42 nM) against purified c-Met kinase activity using ELISA kinase assay. SCC244 has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3. SCC244 strongly suppressed HGF-induced NCI-H441 cell motility and invasion in a dose-dependent manner and was sufficient to block the movement of most cells at a dose of 10 nmol/L.
体内活性	In the MKN-45 model, SCC244 significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively. In addition, tumor stasis was observed following a 21-day treatment with 5 and 10 mg/kg SCC244. Similar results were obtained in the SNU-5 model treated with SCC244, and tumor regression was observed in the high dose group. In the EBC-1 study, all mice receiving SCC244 exhibited a greater than 66.0% decrease in tumor mass, and in both the 10 and 5 mg/kg treatment groups, 1 of 6 mice exhibited no evidence of a tumor. Moreover, in all the tested models, the efficacy of SCC244 at 10 mg/kg is comparable with that of INCB28060 at 15 mg/kg and crizotinib at 50 mg/kg.
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
分子量	459.48
分子式	C21H17N9O2S
CAS No.	1642581-63-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 4.59 mg/mL (10 mM), Sonification is recommended

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1764 mL	10.8819 mL	21.7637 mL	54.4093 mL
	5 mM	0.4353 mL	2.1764 mL	4.3527 mL	10.8819 mL
	10 mM	0.2176 mL	1.0882 mL	2.1764 mL	5.4409 mL

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参考文献

1. Ai J, et al. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：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。

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计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Glumetinib 1642581-63-2 Tyrosine Kinase/Adaptors c-Met/HGFR proliferation tumor cancer SCC244 bioavailable oral HCC inhibit SCC-244 ATP-competitive cell NSCLC Inhibitor SCC 244 inhibitor

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Glumetinib

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