For research use only. Not for therapeutic Use.
CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
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].
| Catalog Number | I005913 |
| CAS Number | 717899-97-3 |
| Synonyms | 1-[5-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)-2-methoxyphenyl]-3-(2,4-dichlorophenyl)urea |
| Molecular Formula | C24H22Cl2N6O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H22Cl2N6O3/c1-12(2)32-10-15(20-22(27)28-11-29-23(20)32)21(33)13-4-7-19(35-3)18(8-13)31-24(34)30-17-6-5-14(25)9-16(17)26/h4-12H,1-3H3,(H2,27,28,29)(H2,30,31,34) |
| InChIKey | VFCRSIORGUNNGT-UHFFFAOYSA-N |
| SMILES | CC(C)N1C=C(C2=C(N=CN=C21)N)C(=O)C3=CC(=C(C=C3)OC)NC(=O)NC4=C(C=C(C=C4)Cl)Cl |
| 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. |
