Lestaurtinib

Cat. No. 3395

Lestaurtinib C26H21N3O4 [111358-88-4]

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Alternative Name: 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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Hexner et al (2008) Lestaurinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood 111 5663. PMID: 17984313.

Weisel et al (2007) Effect of FLT3 inhibition on normal hematopoietic progenitor cells. Ann.N.Y.Acad.Sci. 1106 190. PMID: 17442779.

Miknyoczki et al (1999) 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. Ann.N.Y.Acad.Sci. 880 252. PMID: 10415871.

Gäbler Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J.Cell Mol.Med. 17 265. PMID: 23301855.

If you know of a relevant reference for Lestaurtinib please let us know.

Citations are publications that use Tocris products. Selected citations for Lestaurtinib include:

Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. Eur J Neurosci 10 e0143319. PMID: 26619345.

Deshpande et al (2012) Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26 708. PMID: 21926964.

Do you know of a great paper that uses Lestaurtinib from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: Lestaurtinib, supplier, TrkA, JAK2, FLT3, inhibitors, inhibits, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701, aurora, kinases, AurA, AurB, Tocris Bioscience, JAK Kinase Inhibitor products

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