ce245677

CE-245677 是可逆的Tie2和TrkA B 抑制剂，在细胞体系下的IC50值分别为 4.7 和 1 nM。

CE-245677 is a selective, orally active Tie2 kinase inhibitor identified by Pfizer previously in development for the treatment of certain cancers. CE-245,677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, resp., displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR) and gene family panels, and demonstrates good oral absorption in in vivo rat PK studies (F=80%).