Catalog Number: 3395
Alternate Names: CEP-701
Chemical Name: (9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one
Biological Activity
Potent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM respectively) that prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
  • Storage:
    Desiccate at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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 et al.
    Ann.N.Y.Acad.Sci., 1999;880:252
  2. Effect of FLT3 inhibition on normal hematopoietic progenitor cells.
    Weisel et al.
    Ann.N.Y.Acad.Sci., 2007;1106:190
  3. Lestaurinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.
    Hexner et al.
    Blood, 2008;111:5663

The citations listed below are publications that use Tocris products. Selected citations for Lestaurtinib include:

Showing Results 1 - 2 of 2

  1. Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways.
    Authors: Rogers and Gahring
    Eur J Neurosci
  2. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms.
    Authors: Deshpande Et al.
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