Preferred Label : Casdatifan;
NCIt synonyms : HIF-2a Inhibitor AB521; HIF-2alpha Inhibitor AB521;
NCIt definition : An orally bioavailable allosteric inhibitor of hypoxia inducible factor (HIF)-2alpha,
with potential antineoplastic activity. Upon oral administration, casdatifan targets
and allosterically binds to a hydrophobic pocket on HIF-2alpha leading to a confirmational
change that prevents HIF-2alpha heterodimerization with HIF-1beta and binding to the
hypoxia response element (HRE) binding site on DNA. This results in decreased transcription
and expression of HIF-2alpha downstream target genes, many of which regulate tumor
cell growth and survival. Blocking HIF-2alpha reduces the proliferation of HIF-2alpha-expressing
tumor cells. HIF-2alpha, a heterodimeric transcription factor overexpressed under
hypoxic conditions in many cancer cell types, promotes proliferation, progression
and metastasis of tumors.;
UNII : DP73UWL6LE;
CAS number : 2709069-30-5;
Molecule name : AB 521; AB-521;
NCI Metathesaurus CUI : CL1912584;
Origin ID : C192674;
UMLS CUI : C5785369;
Semantic type(s)
- concept_is_in_subset
- has_target
