Preferred Label : JAK2V617F Inhibitor INCB160058;
NCIt synonyms : JH2 Inhibitor INCB160058; Pseudokinase-targeting Agent INCB160058;
NCIt definition : An orally bioavailable specific pseudokinase (JH2)-binding inhibitor of the Janus-associated
kinase 2 (JAK2) mutation JAK2V617F, with potential antineoplastic activity. Upon oral
administration, JAK2V617F inhibitor INCB160058 selectively targets and binds to the
pseudokinase (JH2) domain of JAK2V617F at the canonical ATP-binding site and inhibits
the activation of JAK2V617F and JAK2V617F-mediated signaling. This may result in the
inhibition of the JAK-STAT signaling pathway and may induce apoptosis in JAK2V617F-overexpressing
cells. The JAK2 mutated form JAK2V617F has a valine-to-phenylalanine modification
at position 617 and plays a key role in tumor cell proliferation and survival. It
is the most common oncogenic driver in myeloproliferative neoplasms (MPNs). INCB160058
does not inhibit wild-type (WT) JAK2.;
Molecule name : INCB-160058; INCB 160058;
NCI Metathesaurus CUI : CL1928466;
Origin ID : C206075;
concept_is_in_subset
- has_target
