CE-245677

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor

Research Areas >> Cancer

Research Areas >> Cardiovascular Disease

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, and displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases, such as KDR, PDGFR, FGFR[1].

CE-245677 shows good oral absorption in in vivo rat PK studies (F=80%)[1].

[1]. Susan LaGreca, et al. Identification of selective, orally active Tie2 kinase inhibitors and discovery of CE-245,677 and PF-371,989. Cancer Research. AACR Annual Meeting-Apr 14-18, 2007.

Entrectinib | LOXO-101 | ANA-12 | LM22B 10 | GW441756 | Repotrectinib | GNF-5837 | Altiratinib | LM22A-4 | Selitrectinib (LOXO-195) | Tyrphostin AG 879 | Belizatinib | Tavilermide | AZ-23 | CH7057288