Catalog No.: PC-42841Not For Human Use, Lab Use Only.
WZ4002 is a potent, mutant-selective, covalent EGFR inhibitor with IC50 of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746-A750 and EGFRE746-A750/T790M, respectively.
WZ4002 is a potent, mutant-selective, covalent EGFR inhibitor with IC50 of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746-A750 and EGFRE746-A750/T790M, respectively.
WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFRT790M mutant alleles.
WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR.
WZ4002 suppresses the growth of erlotinib-resistant tumors caused by gatekeeper T790M mutation combined with Met kinase inhibitor E-7050 in vivo.
