About: JAK2/Src Inhibitor NS-018     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • JAK2/Src Inhibitor NS-018
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • JAK2/Src Inhibitor NS-018
NCI_META_CUI
  • CL430628
PDQ_Open_Trial_Search_ID
  • 710644
PDQ_Closed_Trial_Search_ID
  • 710644
FULL_SYN
  • JAK2/Src Inhibitor NS-018PTNCI
  • NS-018CNNCI
DEFINITION
  • An orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2) and Src-family kinases, with potential antineoplastic activity. JAK2 inhibitor NS-018 competes with ATP for binding to JAK2 as well as the mutated form JAK2V617F, thereby inhibiting the activation of JAK2 and downstream molecules in the JAK2/STAT3 (signal transducer and activator of transcription 3) signaling pathway that plays an important role in normal development, particularly hematopoiesis. In addition, NS-018 inhibits the Src family tyrosine kinases. This eventually leads to the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); JAK2V617F is a constitutively activated kinase that activates the JAK/STAT signaling pathway and dysregulates cell growth and function, and its expression transforms hematopoietic cells to cytokine-independent growth.NCI
code
  • C98109
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