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; 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, also demonstrates strong inhibition on the EGFRC797S activation in the BaF3 cells; 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; demonstrates in vivo monodrug anticancer efficacy in xenograft mouse models
Kinase Assay
Cell Assay
Animal Administration
References
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