生物活性 | |||
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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 | |||
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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 |
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