Preferred Label : Momelotinib Dihydrochloride Monohydrate;
NCIt synonyms : CYT387 Dihydrochloride Monohydrate; N-(Cyanomethyl)-4-(2-{[4-(morpholin-4-yl)phenyl]amino}pyrimidin-4- yl)benzamide Dihydrochloride
Monohydrate;
NCIt definition : The monohydrate 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 : LDX8893L5D;
CAS number : 1841094-17-4;
Drug name : Ojjaara; Omjjara;
NCI Metathesaurus CUI : CL1920455;
Origin ID : C201546;
UMLS CUI : C5850364;
Currated CISMeF NLP mapping
- Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_component_of_chemotherapy_regimen
- is_salt_form_of
