Lestaurtinib

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Cat.No. 3395 - Lestaurtinib | C26H21N3O4 | CAS No. 111358-88-4
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: ≥99% (HPLC)
Datasheet
Citations (2)
Literature
Pathways

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
Storage Desiccate at -20°C
Purity ≥99% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.95 100
ethanol 10.99 25

Preparing Stock Solutions

The following data is based on the product molecular weight 439.46. Batch specific molecular weights may vary from batch to batch due to solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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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View all JAK Kinase Inhibitors

Keywords: Lestaurtinib, supplier, TrkA, JAK2, FLT3, inhibitors, inhibits, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701, aurora, kinases, AurA, AurB, CEP-701, JAK, Kinase, Trk, Receptors, FLT3, Aurora, Kinases, JAK, Kinase, Tocris Bioscience

2 Citations for Lestaurtinib

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

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

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


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Pathways for Lestaurtinib

JAK-STAT

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.