WZ3146 is an irreversiblely inhibitor against EGFR T790M.
Definition
ChEBI: N-[3-[[5-chloro-2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide is a member of piperazines.
Biological Activity
wz3146 is a novel, irreversible inhibitor that specifically inhibits phosphorylation of egfr(l858r0) and egfr(e746_a750) with ic50 values of 2nm each.wz3146 has been reported to inhibit the phosphorylation of egfr in the non–small-cell lung cancer (nsclc) cell lines [1]. wz3146 shows to suppress the growth of egfr t790m containing cell lines. besides, analysis of recombinant egfr t790m kinase incubated with wz3146 by electrospray mass spectrometry revealed stoichiometric addition of one inhibitor molecule to the protein. analysis of a pepsin digest of the modified protein by tandem ms identified cys 797 as the site of modification thus verifying covalent bond formation between wz3146 and egfr [2].
target
EGFR(L858R)
references
[1] thanyanan reungwetwattana, saravut j. weroha, julian r. molina. oncogenic pathways, molecularly targeted therapies, and highlighted
