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Lestaurtinib

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    Lestaurtinib
  • Lestaurtinib
Cat No: 12094
Biochemicals - Kinase Inhibitors
Cayman

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 v...

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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 μM.{21798}
Size 500 µg
Shipping dry ice
CAS Number 111358-88-4
Molecular Formula C26H21N3O4
SMILES O=C(NC1)C2=C1C(C(C=CC=C3)=C3N45)=C4C6=C2C7=C(C=CC=C7)N6[C@@]8([H])C[C@](O)(CO)[C@]5(C)O8
Molecular Weight 439,5
Formulation A crystalline solid
Purity ≥98%
Custom Code 2922.19
UNSPSC code 12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.

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