Lestaurtinib

Cat. No. 3395 7 Citations Submit a Review Datasheet / COA / SDS

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Description: JAK2, FLT3 and TrkA inhibitor; also inhibits AurA and AurB

Alternative 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

Purity: ≥98% (HPLC)

Datasheet

Citations (7)

Reviews

Pathways (1)

Biological Activity Technical Data Solubility Calculators Datasheets References

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

M. Wt	439.46
Formula	C₂₆H₂₁N₃O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	111358-88-4
PubChem ID	126565
InChI Key	UIARLYUEJFELEN-LROUJFHJSA-N
Smiles	O=C(NC3)C1=C3C(C4=CC=CC=C4N5[C@@]78C)=C5C2=C1C6=C(C=CC=C6)N2[C@](O7)(C[C@](CO)8O)[H]

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
Solubility
Solubility	DMSO	20	46

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
0.46 mM	4.95 mL	24.73 mL	49.47 mL
2.3 mM	0.99 mL	4.95 mL	9.89 mL
4.6 mM	0.49 mL	2.47 mL	4.95 mL
23 mM	0.1 mL	0.49 mL	0.99 mL

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Product Datasheets for Lestaurtinib

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for Lestaurtinib

References are publications that support the biological activity of the product.

et al (1999) The novel Ann.N.Y.Acad.Sci. 252 et al (2007) Effect Ann.N.Y.Acad.Sci. 190 et al (2008) Lestaurinib Blood 5663

If class="highlight">Miknyoczki Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits antitumor efficacy against human pancreatic carcinoma (Panc1) xenograft growth and in vivo invasiveness. 880 PMID: 10415871

class="highlight">Weisel of FLT3 inhibition on normal hematopoietic progenitor cells. 1106 PMID: 17442779

class="highlight">Hexner (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. 111 PMID: 17984313

class="highlight">Gäbler effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. 17 PMID: 23301855 you know of a relevant reference for Lestaurtinib, please let us know.

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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:

Pinto et al (2018) Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS One 13 e0207152 PMID: 30419054

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

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

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

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

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

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

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Pathways for Lestaurtinib

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.