| Bioactivity | CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | CE-245677 shows good oral absorption in in vivo rat PK studies (F=80%)[1]. | ||||||||||||
| Name | CE-245677 | ||||||||||||
| CAS | 717899-97-3 | ||||||||||||
| Formula | C24H22Cl2N6O3 | ||||||||||||
| Molar Mass | 513.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |