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JCN037

CAS No. 2305154-31-6

JCN037( —— )

Catalog No. M21982 CAS No. 2305154-31-6

JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    JCN037
  • Note
    Research use only, not for human use.
  • Brief Description
    JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).
  • Description
    JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).Relative to the conventional EGFR TKIs erlotinib and lapatinib, JCN037 displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.
  • In Vitro
    Western Blot Analysis.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.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.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2305154-31-6
  • Formula Weight
    376.18
  • Molecular Formula
    C16H11BrFN3O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (664.58 mM)
  • SMILES
    Fc1c(Br)cccc1Nc1ncnc2cc3OCCOc3cc12
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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.
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