Description
As a novel, mutant-selective EGFR inhibitor, WZ4002 is can inhibit EGFR(L858R) and EGFR(L858R/T790M) with IC50 of 2 nM and 8 nM.
Storage
2 years at -20 centigrade
Targets
EGFR(L858R), EGFR(L858R/T790M)
Molecular Formula
C25H27ClN6O3
Chemical Name
N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide
Solubility
DSMO 13 mg/mL Water
In vitro
As a novel, mutant-selective EGFR inhibitor, WZ4002 is can inhibit EGFR(L858R) and EGFR(L858R/T790M) with IC50 of 2 nM and 8 nM..WZ4002 can inhibit widetype ERBB2 with an IC50 of 32 nM. WZ4002 inhibits EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines.WZ4002 prevents EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR, while the opposite is observed with HKI-272 and gefitinib.
In vivo
WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models.
Download Datasheet