659748-29-5Relevant academic research and scientific papers
Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-Thiazolylquinazolines
Gaul, Micheal D.,Guo, Yu,Affleck, Karen,Cockerill, G. Stuart,Gilmer, Tona M.,Griffin, Robert J.,Guntrip, Stephen,Keith, Barry R.,Knight, Wilson B.,Mullin, Robert J.,Murray, Doris M.,Rusnak, David W.,Smith, Kathryn,Tadepalli, Sarva,Wood, Edgar R.,Lackey, Karen
, p. 637 - 640 (2007/10/03)
We have identified a novel class of 6-thiazolylquinazolines as potent and selective inhibitors of both ErbB-2 and EGFR tyrosine kinase activity, with IC50 values in the nanomolar range. These compounds inhibited the growth of both EGFR (HN5) and ErbB-2 (BT474) over-expressing human tumor cell lines in vitro. Using xenograft models of the same cell lines, we found that the compounds given orally inhibited in vivo tumor growth significantly compared with control animals.
