CE-245677 is a potent, selective, orally active, dual Tie2/Trk kinase inhibitor with IC50 of 4.7 nM, 1 nM for Tie2 and TrkA/B, respectively.
CE-245677 displays >100-fold selectivity against a panel of angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR).
1. Susan LaGreca, et al. Identification of selective, orally active Tie2 kinase inhibitors and discovery of CE-245,677 and PF-371,989. AACR Annual Meeting-Apr 14-18, 2007.
