Preferred Label : Ibrilatazar;
NCIt synonyms : 9,12-Octadecadienoic Acid, 2-Hydroxy-, (9Z,12Z)-; mTORC1/mTORC2/DHFR Inhibitor ABTL0812; 2-Hydroxylinoleic Acid;
NCIt definition : An orally bioavailable, lipid analogue and inhibitor of raptor-mammalian target of
rapamycin (mTOR) (mTOR complex 1; mTORC1), rictor-mTOR (mTOR complex 2; mTORC2) and
dihydrofolate reductase (DHFR) with potential antineoplastic activity. Upon oral administration,
ibrilatazar binds to and inhibits both mTORC1 and mTORC2, which may result in apoptosis
and a decrease in proliferation in mTORC1/2-expressing tumor cells. mTOR is a serine/threonine
kinase that is upregulated in some tumors; it plays an important role in the PI3K/Akt/mTOR
signaling pathway which is often deregulated in cancer cells. In addition, ibrilatazar
inhibits DHFR, an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, thereby
blocking tetrahydrofolate synthesis, and resulting in both the depletion of nucleotide
precursors and the inhibition of DNA, RNA and protein synthesis. This induces autophagy-induced
cell death and further inhibition of cell proliferation.;
UNII : 0DE74TJ7EZ;
CAS number : 57818-44-7;
Molecule name : ABTL0812; SCLN-0812; LP-10218;
NCI Metathesaurus CUI : CL474116;
Origin ID : C117290;
UMLS CUI : C3896929;
Semantic type(s)
UMLS correspondences (same concept)
concept_is_in_subset