WZ3146

Research use only, not for human use.

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).

WZ-3146 is a covalent or irreversible pyrimidine-based EGFR inhibitor against EGFR T790M. WZ-3146 was identified by screening an irreversible kinase inhibitor library specifically against EGFR T790M. WZ-3146 potently suppresses the growth of EGFR-T790M-containing cell lines and inhibits EGFR phosphorylation. WZ-3146 is also effective in murine models of lung cancer driven by EGFR T790M. WZ-3146 may be clinically more effective and better tolerated than quinazoline-based inhibitors. All current EGFR inhibitors possess a structurally related quinazoline-based core scaffold and were identified as ATP-competitive inhibitors of wild-type EGFR.

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WZ3146 | WZ-3146 | WZ 3146

Others

Other Targets

EGFR (E746_A750)| EGFR (E746_A750/T790M)| EGFR (L858R)| EGFR (L858R/T790M)

Cancer

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1214265-56-1

464.95

C24H25ClN6O2

>98% (HPLC)

DMSO : 150 mg/mL. 322.62 mM;

CN1CCN(CC1)C1=CC=C(NC2=NC=C(Cl)C(OC3=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)oxy)phenyl)acrylamide

(-20℃)

With Ice Pack

≥ 2 years