Lestaurtinib

  ( 4 citations )    
Product Datasheet
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
Product Details
Citations (4)
Supplemental Products
Reviews
Biological Activity
Potent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM, respectively). Also inhibits Aurora kinase A and B (IC50 values are 8.1 and 2.3 nM, respectively) and 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:
    439.46
  • Formula:
    C26H21N3O4
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
    >99
  • Storage:
    Desiccate at -20°C
  • CAS No:
    111358-88-4
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.
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Citations:

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

4 Citations: Showing 1 - 4
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  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  2015;10:e0143319
  2. Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F.
    Authors: G&auml;bler Et al.
    J Cell Mol Med  2013;17:265
  3. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms.
    Authors: Deshpande Et al.
    Leukemia  2012;26:708
  4. Impact of gene dosage, loss of wild-type allele, and FLT3 ligand on Flt3-ITD-induced myeloproliferation.
    Authors: Kharazi Et al.
    Blood  2011;118:3613

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