Lestaurtinib

Name: Lestaurtinib
Brand: Tocris Bioscience
SKU: 3395

Tocris Bioscience, part of Bio-Techne | Catalog # 3395

Citations (15)

COA / SDS

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

Key Product Details

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)
Molecular Weight:	439.46

View Full Technical Details for Lestaurtinib

Technical Data
Citations

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 for Lestaurtinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	20

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	0.10 mL	0.49 mL	0.99 mL

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References for Lestaurtinib

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

Weisel Effect of FLT3 inhibition on normal hematopoietic progenitor cells. Ann.N.Y.Acad.Sci. 2007 PMID: 17442779
Hexner Lestaurinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood 2008 PMID: 17984313
Miknyoczki 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. 1999 PMID: 10415871
Gäbler Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J.Cell Mol.Med. PMID: 23301855