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- NCIT_C185891 IAO_0000115 "The citrate salt form of pacritinib, an orally bioavailable inhibitor of Janus kinase 2 (JAK2), the JAK2 mutant JAK2V617F and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration of pacritinib citrate, pacritinib competes with JAK2 and the JAK2 mutant JAK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-signal transducer and activator of transcription (STAT) signaling pathway, and the induction of apoptosis. In addition, pacritinib targets, binds to and inhibits the activity of FLT3. This inhibits FLT3-mediated signaling and the proliferation of FLT3-expressing cancer cells. JAK2, often upregulated or mutated in a variety of cancer cells, plays a key role in tumor cell proliferation and survival. 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. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. In addition, JAK2 and FLT3 play a key role in the regulation of the inflammatory response and dendritic cell (DC) proliferation, differentiation and function. Inhibition of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation of DCs, and may regulate inflammatory and immune responses." @default.
- NCIT_C185891 NCIT_NHC0 "C185891" @default.
- NCIT_C185891 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C185891 NCIT_P108 "Pacritinib Citrate" @default.
- NCIT_C185891 NCIT_P208 "CL1778499" @default.
- NCIT_C185891 NCIT_P210 "1228923-42-9" @default.
- NCIT_C185891 NCIT_P302 "Myelofibrosis With Severe Thrombocytopenia" @default.
- NCIT_C185891 NCIT_P319 "VJ2PH4NXX7" @default.
- NCIT_C185891 NCIT_P322 "FDA" @default.
- NCIT_C185891 NCIT_P322 "GDC" @default.
- NCIT_C185891 NCIT_P399 "609888" @default.
- NCIT_C185891 normalizedInformationContent "95.413332725061409" @default.
- NCIT_C185891 referenceCount "2" @default.
- NCIT_C185891 hasExactSynonym "14,19-Dioxa-5,7,27-triazatetracyclo(19.3.1.12,6.18,12)heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 11-(2-(1-Pyrrolidinyl)Ethoxy)-, 2-Hydroxy-1,2,3-Propanetricarboxylate (1:1)" @default.
- NCIT_C185891 hasExactSynonym "Epjevy" @default.
- NCIT_C185891 hasExactSynonym "PACRITINIB CITRATE" @default.
- NCIT_C185891 hasExactSynonym "Pacritinib Citrate" @default.
- NCIT_C185891 hasExactSynonym "Vonjo" @default.
- NCIT_C185891 inSubset NCIT_C128784 @default.
- NCIT_C185891 inSubset NCIT_C157711 @default.
- NCIT_C185891 inSubset NCIT_C157712 @default.
- NCIT_C185891 inSubset NCIT_C173381 @default.
- NCIT_C185891 inSubset NCIT_C173383 @default.
- NCIT_C185891 inSubset NCIT_C176424 @default.
- NCIT_C185891 inSubset NCIT_C63923 @default.
- NCIT_C185891 type Class @default.
- NCIT_C185891 isDefinedBy ncit.owl @default.
- NCIT_C185891 label "Pacritinib Citrate" @default.
- NCIT_C185891 subClassOf NCIT_C125450 @default.
- NCIT_C185891 subClassOf NCIT_C129824 @default.
- NCIT_C185891 subClassOf NCIT_C129825 @default.
- NCIT_C185891 subClassOf NCIT_C1404 @default.
- NCIT_C185891 subClassOf NCIT_C163758 @default.
- NCIT_C185891 subClassOf NCIT_C172200 @default.
- NCIT_C185891 subClassOf NCIT_C185891 @default.
- NCIT_C185891 subClassOf NCIT_C1908 @default.
- NCIT_C185891 subClassOf NCIT_C1909 @default.
- NCIT_C185891 subClassOf NCIT_C1967 @default.
- NCIT_C185891 subClassOf NCIT_C2189 @default.
- NCIT_C185891 subClassOf NCIT_C274 @default.
- NCIT_C185891 subClassOf NCIT_C471 @default.