JCN037

SKU: orb1298940

Description

JCN037 is a potent, brain-penetrant, non-covalent inhibitor of EGFR, demonstrating high potency against wild-type, phosphorylated wild-type, and phosphorylated EGFRvIII with IC50 values in the low nanomolar range. This profile supports its application in preclinical research for investigating EGFR-driven pathologies, including glioblastoma, in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2305154-31-6
• MW: 376.18
• Purity: >99.99% (May vary between batches)
• Formula: C₁₆H₁₁BrFN₃O₂
• SMILES: Fc1c(Br)cccc1Nc1ncnc2cc3OCCOc3cc12
• Target: EGFR
• Solubility: 10% DMSO+90% Corn Oil:1 mg/mL (2.66 mM);DMSO:10 mg/mL (26.58 mM)

Bioactivity

• Target IC50:
  p-EGFR (WT):3.95 nM |p-EGFR Ⅷ:4.48 nM |EGFR:2.49 nM
• In Vivo:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EGFR, ErbB-1, Epidermal growth factor receptor, HER1, JCN 037, JCN037, JCN-037, JGK 037, JGK037, JGK-037, inhibit, Inhibitor

Compound Identifiers

PubChem CID

138513760