JCN037
产品说明书
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同义名 : | JGK037 |
| CAS号 : | 2305154-31-6 | |
| 货号 : | A1270842 | |
| 分子式 : | C16H11BrFN3O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 376.18 | |
| MDL号 : | N/A | |
| 存储条件： |
Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Epidermal growth factor receptor (EGFR) is altered in almost 50 % of glioblastomas, it currently represents one of the most promising therapeutic targets. EGFR has been associated with several distinct steps in tumorigenesis, from tumor initiation to tumor growth and survival, and also with the regulation of cell migration and angiogenesis[1]. JCN037 is a potent brain-penetrant EGFR inhibitor with IC50 values of 2.49 nM, 3.95 nM and 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ (deletion of exons 2–7 in EGFR), respectively. JCN037 (100-300 nM) potently inhibits the signaling and growth of EGFR-altered patient-derived gliomaspheres: GBM39 (EGFRvIII mutant) and GS025 (amplified EGFR) at levels on par with or better than that of both erlotinib and lapatinib. In vivo, a notable reduction in tumor proliferation was identified in JCN037-treated (300 mg/kg BID) GBM39 tumor-bearing mice, with no significant loss in body weight[2]. | ||
| 作用机制 | The typical type I TKI binding mode occurs, through hydrogen bond interactions with hinge residues and gatekeeper residues mediated through crystallographic water molecule[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.66mL 0.53mL 0.27mL |
13.29mL 2.66mL 1.33mL |
26.58mL 5.32mL 2.66mL |
| 参考文献 |
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