WZ4002

- Overview
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    Background
    
    WZ4002 is a novel mutant-selective epidermal growth factor receptor (EGFR) kinase inhibitor that potently and irreversibly suppresses the ATP-dependent auto-phosphorylation of both wild-type EGFR and EGFR mutants, including EGFR delE746_A750/T790M, EGFR L858R/T790M, EGFR T790M, EGFR delE746_A750 and EGFR L858R, with inhibition constant Ki of 13.6 nM, 1.8 nM, 4 nM, 5 nM, 3.9 nM and 8.5 nM respectively. Although WZ4002 is actively against EGFR mutants rather than wild-type EGFR at lower concentrations resulting in less toxicity in normal tissues, wild-type EGFR is susceptible to higher concentrations of WZ4002 as well as prolonged administration of WZ4002, especially in tissues where it accumulates.
    
    [1]Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J. Noncovalent wild-type-sparing inhibitors of EGFR T790M. Cancer Discov. 2013 Feb;3(2):168-81. doi: 10.1158/2159-8290.CD-12-0357. Epub 2012 Dec 10.
    [2]Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622.
    [3]Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S. 3'-deoxy-3'-18F-fluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and Bcl-xL inhibitors in non-small cell lung cancer. J Nucl Med. 2012 Mar;53(3):443-50. doi: 10.2967/jnumed.111.096503. Epub 2012 Feb 13.
- Properties
  - Alternative Name
    
    N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
    
    CAS Number
    
    1213269-23-8
    
    Molecular Formula
    
    C25H27ClN6O3
    
    Molecular Weight
    
    494.18
    
    Appearance
    
    A solid
    
    Purity
    
    98.89%
    
    Solubility
    
    ≥24.7 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

WZ4002

Background

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