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CAS No.: 1642581-63-2

Glumetinib/葡美替尼（SCC244） Catalog No. CSN24153

Synonyms: SCC244;Gumarontinib

Glumetinib is a novel, potent and highly selective inhibitor of c-Met.

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技术信息

生物活性

描述The receptor tyrosine kinase c-Met plays a critical role in tumor growth, metastasis, tumor angiogenesis, and drug resistance. Glumetinib (SCC244) is an orally bioavailable, small molecule inhibitor of c-Met kinase inhibitor with an IC50 of 0.42 nM. SCC244 is a potent and highly selective inhibitor which displays high selectivity versus 312 other tested protein kinases^[1].In xenografts of human tumor cell lines or non-small cell lung cancer and hepatocellular carcinoma patient-derived tumor tissue driven by MET aberration, SCC244 shows antitumor activity and a superior safety margin. What's more, the in vivo antitumor activity of SCC244 involves the inhibition of c-Met downstream signaling via a mechanism of combined antiproliferation and antiangiogenic effects^[1]. Upon oral administration, SCC244 targets and binds to the c-Met protein, thereby disrupting c-Met-dependent signal transduction pathways. And c-Met inhibitor SCC244 is in clinical trial^[1].
参考文献

[1] Ai J, Chen Y, Peng X, Ji Y, Xi Y, Shen Y, Yang X, Su Y, Sun Y, Gao Y, Ma Y, Xiong B, Shen J, Ding J, Geng M. 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. doi: 10.1158/1535-7163.MCT-17-0368. Epub 2017 Dec 13. PMID: 29237805.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1764 mL
- 10.8818 mL
- 21.7636 mL
- 5 mM
- 0.4353 mL
- 2.1764 mL
- 4.3527 mL
- 10 mM
- 0.2176 mL
- 1.0882 mL
- 2.1764 mL

技术信息

CAS号

1642581-63-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H17N9O2S

运输

蓝冰

分子量

459.48

别名

SCC244;Gumarontinib

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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Glumetinib/葡美替尼（SCC244） Catalog No. CSN24153

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