HKI-357 is a potent, irreversible inhibitor of ErbB2 (HER2) and EGFR with IC50 values of 33 and 34 nM respectively.
HKI-357 inhibits ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations.
HKI-357 demonstrate increased killing of NSCLC cells harboring an EGFR mutation, compared with cells expressing wild-type receptor.
HKI-357 is 10-fold more effective than gefitinib in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation.
