Inhibitor of erbB1 and p56lck
Potent inhibitor of epidermal growth factor receptor erbB1 with IC50 = 0.025 μM.
Potent inhibitor of p56lck with IC50 = 10 μM.
OTAVAchemicals Catalogue Number: 7020540710
CAS Registry Number: N/A
Ref.: Myers et al. The preparation and SAR of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: inhibitors of p56 lck 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 p56 lck and EGF-R tyrosine kinase activity. The most potent inhibitor of p56lck identified, RPR-108518A (10), has an IC50 of 0.50 μM. The 3-chlorophenoxy- and 3-chlorothiophenoxy- derivatives 5 and 6 were also shown to be extremely potent EGF-R inhibitors.