Lestaurtinib

Key Product Details

Product Description

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.

Product Specifications for Lestaurtinib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 17 publications citing the usage of this 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

Product Documents for Lestaurtinib