Lestaurtinib
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
Purity: ≥98%
Biological Activity
Lestaurtinib is a 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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Human papillomavirus E7 oncoprotein increases production of the anti-inflammatory interleukin-18 binding protein in keratinocytes.
Richards, Kathryn, Doble, Rosella, Wasson, Christop, Haider, Mohammed, Blair, G Eric, Wittmann, Miriam, Macdonald, Andrew
J Virol, 2014;88(8):4173-9. -
Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms.
Deshpande A, Reddy MM, Schade GO
Leukemia, 2012;26(4):708-15. -
Synthetic lethal screen demonstrates that a JAK2 inhibitor suppresses a BCL6 dependent IL10RA/JAK2/STAT3 pathway in high grade B-cell lymphoma
Daniel Beck
J Biol Chem, 2016;0(0):. -
Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F.
G?bler
J.Cell Mol.Med., ;17:265 -
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 -
Effect of FLT3 inhibition on normal hematopoietic progenitor cells.
Weisel et al.
Ann.N.Y.Acad.Sci., 2007;1106:190 -
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
Product Datasheets
Citations for Lestaurtinib
The citations listed below are publications that use Tocris products. Selected citations for Lestaurtinib include:
7 Citations: Showing 1 - 7
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Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models.
Authors: Pinto Et al.
PLoS One 2018;13:e0207152
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Synthetic Lethal Screen Demonstrates That a JAK2 Inhibitor Suppresses a BCL6-dependent IL10RA/JAK2/STAT3 Pathway in High Grade B-cell Lymphoma.
Authors: Beck Et al.
J Biol Chem 2016;291:16686
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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
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Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs.
Authors: Gaji Et al.
Antimicrob Agents Chemother 2014;58:2598
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Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F.
Authors: Gäbler Et al.
J Cell Mol Med 2013;17:265
-
Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms.
Authors: Deshpande Et al.
Leukemia 2012;26:708
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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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