CH7233163 is a novel potent, selective mutant EGFR-Del19/T790M/C797S inhibitor with IC50 of 0.28 nM in biochemical assays.
EAI-045, an allosteric EGFR inhibitor, didn't show inhibitory activity in this assay (IC50>1 uM).
CH7233163 potently inhibited the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nM, potently and dose dependently blocked the EGFR phosphorylation.
CH7233163 more selectively inhibits various types of EGFR mutants (e.g., L858R/T790M/C797S, L858R/T790M, Del19/T790M, Del19, and L858R) over wild type.
CH7233163 potently inhibited not only EGFR-Del19/T790M/C797S but also various EGFR mutations, including L858R/T790M/C797S triple mutations, double mutations and single-activating-mutations.
