Cat. No. 3395
Alternative Name: CEP-701
Chemical Name: (9S,10S,12R)-2,3,9,10,11,12-Hexahyd
Biological ActivityPotent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM respectively) that 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.
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.
Certificate of Analysis / Safety Data Sheet
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.
Weisel et al (2007) Effect of FLT3 inhibition on normal hematopoietic progenitor cells. Ann.N.Y.Acad.Sci. 1106 190. PMID: 17442779.
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.
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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.
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Keywords: Lestaurtinib, supplier, TrkA, JAK2, FLT3, inhibitors, inhibits, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701, Tocris Bioscience, JAK Inhibitor products
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