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JND3229

Chemical Structure : JND3229

CAS No.: 2260886-64-2

JND3229 (JND-3229;JND 3229)

Catalog No.: PC-35826Not For Human Use, Lab Use Only.

JND3229 (JND-3229) is a novel highly potent, reversible EGFR C797S mutant inhibitor, potently inhibits the kinase activities of EGFRL858R/T790M and EGFRL858R/T790M/C797 with IC50 of 5.8 nM and 30.5 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JND3229 (JND-3229) is a novel highly potent, reversible EGFR C797S mutant inhibitor, potently inhibits the kinase activities of EGFRL858R/T790M and EGFRL858R/T790M/C797 with IC50 of 5.8 nM and 30.5 nM, respectively.
JND3229 inhibits WT EGFR with IC50 of 6.8 nM, JND3229 potently inhibits the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in a dose-dependent manner in cell-based assays.
JND3229 also demonstrates strong inhibition on the EGFRC797S activation in the BaF3 cell.
JND3229 inhibits the proliferation of BaF3 cells harboring the EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S mutations with IC50 values of 0.51 and 0.32 µM, respectively.
JND3229 demonstrates in vivo monodrug anticancer efficacy in xenograft mouse models.

Physicochemical Properties

M.Wt 617.195
Formula C33H41ClN8O2
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-((1r,4r)-4-(3-(2-chlorophenyl)-7-((3-methyl-4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)cyclohexyl)propionamide

References

1. Lu X, et al. ACS Med Chem Lett. 2018 Oct 8;9(11):1123-1127.

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