Preferred Label : Eltanexor;
NCIt synonyms : XPO1-inhibiting SINE Compound KPT-8602; (2E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)prop-2-enamide; Selective Inhibitor of Nuclear Export KPT-8602; Exportin 1 Inhibitor KPT-8602;
NCIt definition : An orally bioavailable inhibitor of exportin-1 (XPO1; chromosome region maintenance
1 protein homolog; CRM1), with potential antineoplastic activity. Upon administration,
eltanexor binds to the XPO1 cargo binding site, which prevents the XPO1-mediated nuclear
export of cargo proteins such as tumor suppressor proteins (TSPs), including p53,
p73, BRCA1/2, pRB, FOXO, and other growth regulatory proteins and leads to their selective
accumulation in the nuclei of tumor cells. As a selective inhibitor of nuclear export
(SINE), KPT-8602 restores the nuclear localization and function of tumor suppressing
proteins which leads to the induction of apoptosis in tumor cells. XPO1, the major
export factor that transports proteins from the nucleus to the cytoplasm, is overexpressed
in a variety of cancer cell types while minimally expressed in normal, healthy cells.
The export of tumor suppressor proteins into the cytoplasm prevents them from initiating
apoptosis and leads to uncontrolled tumor cell proliferation.;
UNII : Q59IQJ9NTK;
InChIKey : JFBAVWVBLRIWHM-AWNIVKPZSA-N;
CAS number : 1642300-52-4; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1642300-52-4
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G-SRS /a ;
Molecule name : KPT-8602; ATG-016; ATG 016;
NCI Metathesaurus CUI : CL504007;
Origin ID : C125193;
UMLS CUI : C4682412;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
