R&D Systems Inc. Tocris Bioscience Boston Biochem

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) 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:
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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

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.

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

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.

If you know of a relevant citation for this product please let us know.

Keywords: Lestaurtinib, supplier, TrkA, JAK2, FLT3, inhibitors, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701

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