EGFR (HER1) Inhibitor
     
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EGFR (HER1) Inhibitor

6,7-dimethoxy-N-(4-methoxyphenyl)-quinazolin-4-amine 

Potent inhibitor of epidermal growth factor receptor erbB1 with IC50 = 0.25 ?M.

Potent inhibitor of p56lck with IC50 = 10 ?M.

nw-egfr_inhibitor4

OTAVAchemicals Catalogue Number:   7015070078

CAS Registry Number:  N/A

Purity: 99%

Ref.: Myers et al.  The preparation and  SAR of  4-(anilino),  4-(phenoxy), and 4-(thiophenoxy)-quinazolines: inhibitors of  p56lck  and  EGF-R tyrosine kinase activity. Bioorg. Med. Chem. Lett.,  (1997) Vol.  7,  No.  4,  pp.  417-420.                                            

Abstract: We report herein our preliminary results  of a SAR study of quinazoline-based  inhibitors of p56lck and EGF-R tyrosine kinase activity.  The most potent inhibitor of p56lck  identified, RPR-108518A (10),  has an IC50 of  0.50  ?M.  The  3-chlorophenoxy-  and  3-chlorothiophenoxy-  derivatives  5  and  6  were  also  shown to  be extremely potent EGF-R inhibitors.

 
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