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.

Product information

CAS Number: 2305154-31-6

Molecular Weight: 376.18

Formula: C16H11BrFN3O2

Chemical Name: N-(3-bromo-2-fluorophenyl)-7H,8H-[1,4]dioxino[2,3-g]quinazolin-4-amine

Smiles: FC1=C(Br)C=CC=C1NC1=NC=NC2=CC3OCCOC=3C=C21

InChiKey: MTLUFWWVOINWEL-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (664.58 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JCN037 exhibits GI50 values of 329 nM and 1116 nM in HK301 cells and GBM39 cells, respectively.

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.

Products are for research use only. Not for human use.