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Biological Activity for Lestaurtinib
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 for Lestaurtinib
|Storage||Desiccate at -20°C|
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.
Solubility Data for Lestaurtinib
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Lestaurtinib
The following data is based on the product molecular weight 439.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.28 mL||11.38 mL||22.76 mL|
|5 mM||0.46 mL||2.28 mL||4.55 mL|
|10 mM||0.23 mL||1.14 mL||2.28 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References for Lestaurtinib
References are publications that support the biological activity of the product.
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
Gäbler Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J.Cell Mol.Med. 17 265 PMID: 23301855
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Keywords: Lestaurtinib, Lestaurtinib supplier, TrkA, JAK2, FLT3, inhibitors, inhibits, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701, aurora, kinases, AurA, AurB, CEP-701, JAK, Kinase, Trk, Aurora, 3395, Tocris Bioscience
7 Citations for Lestaurtinib
Citations are publications that use Tocris products. Selected citations for Lestaurtinib include:
Gäbler et al (2013) Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J Cell Mol Med 17 265 PMID: 23301855
Deshpande et al (2012) Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26 708 PMID: 21926964
Kharazi et al (2011) Impact of gene dosage, loss of wild-type allele, and FLT3 ligand on Flt3-ITD-induced myeloproliferation. Blood 118 3613 PMID: 21813452
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
Gaji et al (2014) Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother 58 2598 PMID: 24550330
Pinto et al (2018) Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS One 13 e0207152 PMID: 30419054
Beck et al (2016) Synthetic Lethal Screen Demonstrates That a JAK2 Inhibitor Suppresses a BCL6-dependent IL10RA/JAK2/STAT3 Pathway in High Grade B-cell Lymphoma. J Biol Chem 291 16686 PMID: 27268052
Do you know of a great paper that uses Lestaurtinib from Tocris? Please let us know.
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Literature in this Area
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