详情描述
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.
Product information
CAS Number: 1214265-56-1
Molecular Weight: 464.95
Formula: C24H25ClN6O2
Synonym:
WZ-3146
Chemical Name: N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide
Smiles: CN1CCN(CC1)C1C=CC(=CC=1)NC1=NC(OC2=CC(=CC=C2)NC(=O)C=C)=C(Cl)C=N1
InChiKey: APHGZZPEOCCYNO-UHFFFAOYSA-N
InChi: InChI=1S/C24H25ClN6O2/c1-3-22(32)27-18-5-4-6-20(15-18)33-23-21(25)16-26-24(29-23)28-17-7-9-19(10-8-17)31-13-11-30(2)12-14-31/h3-10,15-16H,1,11-14H2,2H3,(H,27,32)(H,26,28,29)
Technical Data
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
In Vitro:
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.
References:
- Zhou W, et al. Nature, 2009, 462(7276), 1070-1074.
Products are for research use only. Not for human use.