Lestaurtinib

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 2,3,9S,10S,11,12R-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
• Correlated keywords
  • 156256-78-9 A154475.0 A-154475.0 KT5555 KT-5555 SP-924 SP924 CEP-701 CEP701 Janus-associated kinase JAKs receptors tyrosine kinase JAK2V617F myeloproliferative disorders JAK2 inhibitors STAT5 STAT3 cancers PRK1 PNK1 trkB inhibits inhibitions straurosporine analogs JAK-2 STAT-5 STAT-3 STATs erythroleukemic PRK-1 PNK-1 PRKs PNKs histones H3 threonine 11 androgen-dependent genes prostate
• Product Overview:
  Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} A JAK2 gene fusion mutation, JAK2V617F, that causes unchecked activation of various growth factors and cytokines, has been linked to myeloproliferative disorders.{21781} Lestaurtinib is a staurosporine analog that potently inhibits JAK2 kinase (IC50 = 1 nM) and downstream targets STAT5 (IC50 = 10-30 nM) and STAT3 in a human erythroleukemic cell line expressing the JAK2V617F mutation.{21781,21796} It has been used to reduce tumor growth in a xenograft model of pancreatic ductal adenocarcinoma, to inhibit cell growth in a trk-B overexpressing neuroblastoma xenograft model, and to block proliferation and induce apoptosis in Hodgkin lymphoma cell lines.{21794,21797,21795} Lestaurtinib has since been reported to potently inhibit the epigenetic kinase PRK1 in vitro (IC50 = 8.6 nM), inducing hypophosphorylation of histone H3 threonine 11 and blocking androgen-dependent gene expression in prostate cancer cells at a concentration of 5 ?M.{21798}