Preferred Label : Pacritinib;
NCIt synonyms : Oral JAK2 Inhibitor SB1518; JAK2 Inhibitor SB1518;
NCIt definition : 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, 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.;
UNII : G22N65IL3O;
InChIKey : HWXVIOGONBBTBY-ONEGZZNKSA-N;
CAS number : 937272-79-2;
Molecule name : SB-1518; SB 1518;
Chemical formula : C28H32N4O3;
Codes from synonyms : 380;
Origin ID : C78837;
UMLS CUI : C3467842;
Automatic exact mappings (from CISMeF team)
- 11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,26-triazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene [MeSH Supplementary Concept]
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
