CE-245677

CAS No. 717899-97-3

CE-245677( CE245677 )

Catalog No. M15745 CAS No. 717899-97-3

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 71 Get Quote
5MG 110 Get Quote
10MG 177 Get Quote
25MG 296 Get Quote
50MG 410 Get Quote
100MG 605 Get Quote
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Biological Information

  • Product Name
    CE-245677
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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; displays >100-fold selectivity against a panel of angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR).Pain Phase 1 Clinical.
  • In Vitro
    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.
  • In Vivo
    CE-245677 shows good oral absorption in in vivo rat PK studies (F=80%).
  • Synonyms
    CE245677
  • Pathway
    Tyrosine Kinase
  • Target
    Angiopoietin Receptor
  • Recptor
    Angiopoietin Receptor
  • Research Area
    Neurological Disease
  • Indication
    Pain

Chemical Information

  • CAS Number
    717899-97-3
  • Formula Weight
    513.379
  • Molecular Formula
    C24H22Cl2N6O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (243.48 mM)
  • SMILES
    O=C(NC1=CC=C(Cl)C=C1Cl)NC2=CC(C(C3=CN(C(C)C)C4=NC=NC(N)=C43)=O)=CC=C2OC
  • Chemical Name
    1-(5-(4-amino-7-isopropyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonyl)-2-methoxyphenyl)-3-(2,4-dichlorophenyl)urea

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.
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