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). 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.
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
  4. Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F.
    G?bler
    J.Cell Mol.Med., ;17:265
Citations:

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

2 Citations: Showing 1 - 2
Filter your results:

  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. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms.
    Authors: Deshpande Et al.
    Leukemia 2012;26:708

Have you used Lestaurtinib?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

or select another batch: 

Feedback

Customer Information