Preferred Label : Momelotinib Dihydrochloride;
NCIt definition : The dihydrochloride salt form of momelotinib, an orally bioavailable small molecule
inhibitor of wild-type (WT) Janus kinases 1 and 2 (JAK1/2), the JAK2 mutant form JAK2V617F,
and activin A receptor type 1 (ACVR1; activin receptor like kinase 2; ALK2), with
antineoplastic activity. Upon oral administration, momelotinib competes with JAK1/2
for ATP binding, which results in inhibition of JAK1/2 activation, inhibition of the
JAK-STAT signaling pathway, and leads to the induction of apoptosis and a reduction
of tumor cell proliferation in JAK1/2-expressing tumor cells. In addition, the inhibition
of ALK2 prevents liver hepcidin formation, increases iron availability and increases
red blood cell (RBC) production. 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.;
UNII : RBH995N496;
InChIKey : IPNATXQRPWRHKD-UHFFFAOYSA-N;
CAS number : 1380317-28-1; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1380317-28-1
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G-SRS /a ;
NCI Metathesaurus CUI : CL1382668;
Origin ID : C170191;
UMLS CUI : C5418464;
Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_salt_form_of
