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; potently inhibits the epigenetic kinase PRK1 (PKN1) in vitro (IC50 = 8.6 nM)

Lestaurtinib – 500 µg

Brand:
Cayman
CAS:
111358-88-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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 μM.{21798}  

 

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Description

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; potently inhibits the epigenetic kinase PRK1 (PKN1) in vitro (IC50 = 8.6 nM)

Formal name: 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

Synonyms:  A 154475.0|CEP-701|KT 5555|SP 924

Molecular weight: 439.5

CAS: 111358-88-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cell Biology|Cell Signaling|JAK Signaling||Research Area|Epigenetics, Transcription, & Translation

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