WZ8040

Research use only, not for human use.

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. WZ8040 is about 30-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than other quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ-8040 may be clinically more effective and better tolerated than quinazoline-based inhibitors.

WZ8040 exhibits IC50 values of 1 nM for HCC827 (EGFR Del E746_A750), 6 nM for PC9 (EGFR Del E746_A750), 66 nM for H3255 (EGFR L858R), 9 nM for H1975 (EGFR L858R/T790M), 8 nM for PC9 GR (EGFR Del E746_A750/T790M), >3.3 μM for HCC827 GR (EGFR E746_A750/MET amp), 738 nM for H1819 (ERBB2 amp), 915 nM for Calu-3 (ERBB2 amp), 744 nM for H1781 (ERBB2 Ins G776V, C), 1.82 μM for HN11 (EGFR & ERBB2 WT), respectively. Western Blot Analysis Cell Line:NSCLC cell lines and Ba/F3 cells.Concentration: 0-3.3 μM.Incubation Time:24 hours.Result:Exhibited activity for EGFR-mutated NSCLC lines, such as HH827, PC9, H3255, H1819, Calu-3, H1781 and HN11 cells.

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WZ8040 | WZ8040 | WZ 8040

Cytoskeleton/Cell Adhesion Molecules

Kinesin

EGFR (T790M)

Cancer

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1214265-57-2

481.01

C24H25ClN6OS

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (51.97 mM)

CN1CCN(CC1)C1=CC=C(NC2=NC=C(Cl)C(SC3=CC(NC(=O)C=C)=CC=C3)=N2)C=C1

N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylamide

(-20℃)

With Ice Pack

≥ 2 years