Glumetinib

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Chemical Structure| 1642581-63-2 同义名 : Gumarontinib; SCC244
CAS号 : 1642581-63-2
货号 : A1154012
分子式 : C21H17N9O2S
纯度 : 99%+
分子量 : 459.48
MDL号 : MFCD31693844
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL

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.