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JCN037

Chemical Structure : JCN037

CAS No.: 2305154-31-6

JCN037 (JCN 037, JGK037)

Catalog No.: PC-38187Not For Human Use, Lab Use Only.

JCN037 (JCN 037, JGK037) is novel potent, brain-penetrant, noncovalent EGFR TKI with IC50 of 2.49 nM.

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Biological Activity

JCN037 (JCN 037, JGK037) is novel potent, brain-penetrant, noncovalent EGFR TKI with IC50 of 2.49 nM.
JCN037 demonstrated both nanomolar potency against both mutant EGFRvIII and wtEGFR in cellular assays (IC50=3.85 and 4.48 nM, respectively) and greater than 2:1 brain to plasma levels.
JCN037 shows high inhibitory activity against EGFRvIII mutant patient derived GBM cells, HK301 and GBM39, which is more potent than Erlotinib and Lapatinib.
JCN037 displays superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.

Physicochemical Properties

M.Wt 376.185
Formula C16H11BrFN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-bromo-2-fluorophenyl)-7,8-dihydro-[1,4]dioxino[2,3-g]quinazolin-4-amine

References

1. Jonathan E Tsang, et al. ACS Med Chem Lett. 2020 May 1;11(10):1799-1809.

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