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AttributesValues
rdf:type
rdfs:label
  • Momelotinib
rdfs:subClassOf
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Momelotinib
NCI_META_CUI
  • CL413566
CAS_Registry
  • 1056634-68-4
FDA_UNII_Code
  • 6O01GMS00P
Contributing_Source
  • FDA
PDQ_Open_Trial_Search_ID
  • 660135
PDQ_Closed_Trial_Search_ID
  • 660135
Chemical_Formula
  • C23H22N6O2
FULL_SYN
  • JAK1/2 Inhibitor CYT387SYNCI
  • MomelotinibPTNCI
  • CYT387CNNCI
  • MOMELOTINIBPTFDA6O01GMS00P
  • N-(Cyanomethyl)-4-(2-((4-(morpholin-4-yl)phenyl)amino)pyrimidin-4-yl)benzamideSNNCI
DEFINITION
  • An orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with potential antineoplastic activity. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity and is often dysregulated in a variety of tumor cell types.NCI
code
  • C88311
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