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JCN037

Names

[ CAS No. ]:
2305154-31-6

[ Name ]:
JCN037

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[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]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H11BrFN3O2

[ Molecular Weight ]:
376.18

Related Compounds