Preferred Label : Fedratinib;
NCIt synonyms : Benzenesulfonamide, N-(1,1-dimethylethyl)-3-((5-methyl-2-((4-(2-(1-pyrrolidinyl)ethoxy)phenyl)amino)-4-pyrimidinyl)amino)-;
NCIt definition : 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 : 6L1XP550I6;
InChIKey : JOOXLOJCABQBSG-UHFFFAOYSA-N;
CAS number : 936091-26-8;
Molecule name : SAR-302503; SAR 302503; TG-101348; TG 101348;
Codes from synonyms : 48561;
Origin ID : C88293;
UMLS CUI : C3886623;
Currated CISMeF NLP mapping
- See also inter- (CISMeF)
- Semantic type(s)
- UMLS correspondences (same concept)
- Validated automatic mappings to BTNT
- concept_is_in_subset
- has_salt_form
- has_target
- is_component_of_chemotherapy_regimen
- is_free_acid_or_base_form_of
