2305154-31-6
2305154-31-6 structure
- Name: JCN037
- Chemical Name: JCN037
- CAS Number: 2305154-31-6
- Molecular Formula: C16H11BrFN3O2
- Molecular Weight: 376.18
- Catalog: Signaling Pathways JAK/STAT Signaling EGFR
- Create Date: 2020-08-11 17:00:05
- Modify Date: 2024-01-08 00:30:59
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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[1].
| Name | JCN037 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
2.49 nM (EGFR), 3.95 nM (p-wtEGFR), 4.48 nM (pEGFRvⅢ)[1]. |
| In Vitro | JCN037 exhibits GI50 values of 329 nM and 1116 nM in HK301 cells and GBM39 cells, respectively[1]. Western Blot Analysis[1]. Cell Line: GBM39 and GS025 cells. Concentration: 0-3333 nM Incubation Time: Result: Downregulated pEGFRvⅢ, p Akt, p-ERK, and p-S6 protein levels, significantly. |
| In Vivo | JCN037 (compound 5) exhibits low oral bioavailability due to a rapid hydroxylation of the fused 1,4-dioxane ring, suggesting first pass metabolism[1]. 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[1]. |
| References |
| Molecular Formula | C16H11BrFN3O2 |
|---|---|
| Molecular Weight | 376.18 |