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.
CAS Number: 1214265-56-1
Molecular Weight: 464.95
Chemical Name: N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del E746_A750 containing HCC827 cells, 15 nM in EGFR Del E746_A750 containing PC9 cells, 29 nM in EGFR L858R/T790M containing H1975 cells and 3 nM in EGFR Del E746_A750/T790M containing PC9 GR cells.
- Zhou W, et al. Nature, 2009, 462(7276), 1070-1074.
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