Preferred Label : Fedratinib Hydrochloride;
NCIt synonyms : Fedratinib Dihydrochloride Monohydrate; N-tert-butyl-3-((5-methyl-2-((4-(2-pyrrolidin-1-ylethoxy)phenyl)amino)pyrimidin-4-yl)amino)
Benzenesulfonamide Dihydrochloride Monohydrate; Benzenesulfonamide, N-(1,1-Dimethylethyl)-3-((5-methyl-2-((4-(2-(1-pyrrolidinyl)ethoxy)phenyl)amino)-4-pyrimidinyl)amino)-,
Hydrochloride, Hydrate (1:2:1);
NCIt definition : The monohydrate dihydrochloride salt form of fedratinib, an orally bioavailable, small-molecule,
ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) and FMS-like tyrosine
kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral
administration, fedratinib competes with wild-type JAK2 as well as mutated forms for
ATP binding, which may result in inhibition of JAK2 activation, inhibition of the
JAK-STAT signaling pathway, inhibition of tumor cell proliferation and induction of
tumor cell apoptosis. JAK2 is the most commonly mutated gene in bcr-abl-negative myeloproliferative
disorders (MPDs). In addition, fedratinib targets, binds to and inhibits the activity
of FLT3. This inhibits uncontrolled FLT3 signaling and results in the inhibition of
proliferation in tumor cells overexpressing FLT3. FLT3, a class III receptor tyrosine
kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute
myeloid leukemias and plays a key role in tumor cell proliferation.;
UNII : UH9J2HBQWJ;
InChIKey : QAFZLTVOFJHYDF-UHFFFAOYSA-N;
CAS number : 1374744-69-0;
Drug name : Inrebic;
Molecule name : SAR302503a;
NCI Metathesaurus CUI : CL973405;
Origin ID : C162995;
UMLS CUI : C5196154;
Currated CISMeF NLP mapping
Semantic type(s)
UMLS correspondences (same concept)
concept_is_in_subset
has_free_acid_or_base_form
has_target
is_salt_form_of