| 产品描述： | JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively |
| 靶点： |
2.49 nM (EGFR), 3.95 nM (p-wtEGFR), 4.48 nM (pEGFRvⅢ) |
| 体内研究： |
JCN037 (compound 5) exhibits low oral bioavailability due to a rapid hydroxylation of the fused 1,4-dioxane ring, suggesting first pass metabolism. JCN037 (compound 5, 300 mg/kg, BID) treatment provides a significant survival benefit, whereby median survival increased by 47% from 37.5 days to 55 days with 5 treatment |
| 参考文献： |
1. Jonathan E. Tsang, et al. Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. ACS Med. Chem. Lett. 2020. May 1. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.658 ml |
13.291 ml |
26.583 ml |
| 5 mM |
0.532 ml |
2.658 ml |
5.317 ml |
| 10 mM |
0.266 ml |
1.329 ml |
2.658 ml |
| 50 mM |
0.053 ml |
0.266 ml |
0.532 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
