Lestaurtinib

(HB1429)

Product overview

  • Name
    Lestaurtinib
  • Short description
    Potent, non-selective tyrosine kinase inhibitor
  • Biological description
    Potent and non-selective tyrosine kinase inhibitor. Inhibits JAK2 and JAK3 (IC50 values are 0.9 and 3 nM respectively). Also inhibits TrkA, TrkB, TrkC and FLT3 and prevents phosphorylation of STAT5. Shows anti-proliferative and anti-tumor actions.
  • Alternative names
    CEP-701; KT-5555
  • Biological action
    Inhibitor
  • Purity
    >99%
  • Our products in action

Properties

  • Chemical name
    (9S,10S,12R)-2,3,9,10,11,12-Hexahyd ro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epo xy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1, 6]benzodiazocin-1-one
  • Molecular Weight
    439.46
  • Chemical structure
    Lestaurtinib  [111358-88-4]
  • Molecular Formula
    C26H21N3O4
  • CAS Number
    111358-88-4

Storing and Using Your Product

  • Storage instructions
    -20°C (desiccate)
  • Solubility overview
    soluble in DMSO (100mM) or ethanol (25mM)

References for Lestaurtinib

  • Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.

    Hexner EO et al (2008) Blood 111(12) : 5663-71.
    PubMedID: 17984313
  • Effect of FLT3 inhibition on normal hematopoietic progenitor cells.

    Weisel KC et al (2007) Ann N Y Acad Sci 1106 : 190-6.
    PubMedID: 17442779
  • The novel Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits antitumor efficacy against human pancreatic carcinoma (Panc1) xenograft growth and in vivo invasiveness.

    Miknyoczki SJ et al (1999) Ann N Y Acad Sci 880 : 252-62.
    PubMedID: 10415871
  • Lestaurtinib enhances the antitumor efficacy of chemotherapy in murine xenograft models of neuroblastoma.

    Iyer R et al (2010) Clin Cancer Res 16(5) : 1478-85.
    PubMedID: 20179224

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