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Version: 16.11d (Release date: 2016-11-28)
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JAK2/Src Inhibitor NS-018 (Code C98109)

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Terms & Properties

Preferred Name: JAK2/Src Inhibitor NS-018

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.

Display Name: JAK2/Src Inhibitor NS-018

Label: JAK2/Src Inhibitor NS-018

NCI Thesaurus Code: C98109 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL430628  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
JAK2/Src Inhibitor NS-018
NS-018

External Source Codes: 
PDQ Closed Trial Search ID 710644
PDQ Open Trial Search ID 710644 (check for NCI PDQ open clinical trial info)
NCI META CUI CL430628

Other Properties:
Name Value (qualifiers indented underneath)
code C98109
Contributing_Source CTRP
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C98109

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