Lestaurtinib

• Supplier: Tocris Bioscience
• Catalog: 2959
• Prices: $279.00
• Sizes: 1 mg
• Function Type: Inhibitor
• Cas Number: 111358-88-4
• 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
• Formula: C26H21N3O4
• Molecular Weight: 439.46
• Purity: >99 %
• Description: Potent JAK2, FLT3 and TrkA inhibitor (IC 50 values are 0.9, 3 and < 25 nM, respectively). Also inhibits Aurora kinase A and B (IC 50 values are 8.1 and 2.3 nM, respectively) and prevents STAT5 phosphorylation (IC 50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC 50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo .

Product References

The novel Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits - The novel Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits

Miknyoczki SJ, Dionne CA, Klein-Szanto AJ, Ruggeri BA. Ann N Y Acad Sci. 1999 Jun 30;880:252-62.

Effect of FLT3 inhibition on normal hematopoietic progenitor cells. - Effect of FLT3 inhibition on normal hematopoietic progenitor cells.

Weisel KC, Yildirim S, Schweikle E, Kanz L, Mohle R. Ann N Y Acad Sci. 2007 Jun;1106:190-6. Epub 2007 Apr 18.

Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling - Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling

Hexner EO, Serdikoff C, Jan M, Swider CR, Robinson C, Yang S, Angeles T, Emerson SG, Carroll M, Ruggeri B, Dobrzanski P. Blood. 2008 Jun 15;111(12):5663-71. Epub 2007 Nov 5.