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Version: 17.06d (Release date: 2017-06-26)
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JAK2 Inhibitor WP1066 (Code C111042)

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Terms & Properties

Preferred Name: JAK2 Inhibitor WP1066

Definition: An orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. Upon oral administration, WP1066 specifically binds to both JAK2 and its mutated form JAK2 V617F, and inhibits their phosphorylation and activation. In addition, this agent degrades JAK2 protein. This results in the inhibition of the JAK- signal transducer and activator of transcription (STAT) and phosphoinositide-3-kinase (PI3K)/AKT signaling pathways, resulting in the induction of apoptosis in tumor cells overexpressing JAK2. JAK2, a tyrosine kinase, is overexpressed in a variety of tumor cells and is correlated with increased tumor cell proliferation and survival. The mutated form JAK2 V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival.

Label: JAK2 Inhibitor WP1066

NCI Thesaurus Code: C111042 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1957161  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
(E)-3(6-bromopyridin-2-yl)-2-cyano-N-((S0-1-phenylethyl)acrylamide
JAK2 Inhibitor WP1066
WP1066

External Source Codes: 
CAS Registry Number 857064-38-1 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 751888
PDQ Open Trial Search ID 751888 (check for NCI PDQ open clinical trial info)
UMLS CUI C1957161

Other Properties:
     Name Value (qualifiers indented underneath)
code C111042
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=C111042

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