AZ-5104 (GMP)

GMP-grade AZ-5104 potently inhibits the enzymatic activities of recombinant mutant and wild-type EGFR, and exhibits reduced selectivity for mutant EGFR compared with AZD9291^[2].
AZ-5104 GMP exhibits no significant activity against the IGF-1R receptor family in cellular assays^[2].
AZ-5104 GMP (incubated for 6 h) potently inhibits the phosphorylation of rare EGFR mutants (EGFR^G719S, EGFR^L861Q, exon 19 insertion mutation, EGFR^vIII) in transfected HEK293 cells, with activity superior to that of AZD9291, but exerts no inhibitory effect on EGFR exon 20 insertion mutation^[2].
AZ-5104 GMP exhibits stronger activity than AZD9291 in inhibiting HER2 phosphorylation in cellular assays^[2].
AZ-5104 GMP (2 nM-33 nM; 2 h) potently inhibits EGFR phosphorylation in PC-9, H1975 and LOVO human lung cancer cell lines, and exhibits reduced selectivity for mutant EGFR over wild-type EGFR compared with AZD9291^[2].
AZ-5104 GMP (administered for 3 days) exhibits stronger activity than AZD9291 in inhibiting the proliferation of EGFR-mutant and wild-type human lung cancer cell lines in vitro^[2].
AZ-5104 GMP exhibits greater potency than AZD9291 in inhibiting the growth and signal transduction of human lung cancer cells harboring HER2 exon 20 mutations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.