For research use only. Not for therapeutic Use.
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].
JCN037 exhibits GI50 values of 329 nM and 1116 nM in HK301 cells and GBM39 cells, respectively[1].
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].
| Catalog Number | I015199 |
| CAS Number | 2305154-31-6 |
| Synonyms | N-(3-bromo-2-fluorophenyl)-7,8-dihydro-[1,4]dioxino[2,3-g]quinazolin-4-amine |
| Molecular Formula | C16H11BrFN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H11BrFN3O2/c17-10-2-1-3-11(15(10)18)21-16-9-6-13-14(23-5-4-22-13)7-12(9)19-8-20-16/h1-3,6-8H,4-5H2,(H,19,20,21) |
| InChIKey | MTLUFWWVOINWEL-UHFFFAOYSA-N |
| SMILES | C1COC2=C(O1)C=C3C(=C2)N=CN=C3NC4=C(C(=CC=C4)Br)F |
| Reference | [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. |
