Preferred Label : Pimitespib;
NCIt synonyms : Heat Shock Protein 90 alpha/beta Inhibitor TAS-116; HSP90alpha/beta Inhibitor TAS-116; 3-Ethyl-4-(3-(1-methylethyl)-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo(3,4-b)pyridin-1-yl)benzamide;
NCIt definition : A specific inhibitor of heat shock protein 90 (Hsp90) subtypes alpha and beta, with
potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration,
pimitespib specifically binds to and inhibits the activity of Hsp90 alpha and beta;
this results in the proteasomal degradation of oncogenic client proteins, which inhibits
client protein dependent-signaling, induces apoptosis, and inhibits the proliferation
of cells overexpressing HSP90alpha/beta. Hsp90, a family of molecular chaperone proteins
that are upregulated in a variety of tumor cells, plays a key role in the conformational
maturation, stability, and function of client proteins within the cell,; many of which
are involved in signal transduction, cell cycle regulation and apoptosis, including
kinases, cell-cycle regulators, transcription factors and hormone receptors. As TAS-116
selectively inhibits cytosolic HSP90alpha and beta only and does not inhibit HSP90
paralogs, such as endoplasmic reticulum GRP94 or mitochondrial TRAP1, this agent may
have less off-target toxicity as compared to non-selective HSP90 inhibitors.;
UNII : PLO044MUDZ;
InChIKey : NVVPMZUGELHVMH-UHFFFAOYSA-N;
CAS number : 1260533-36-5;
Molecule name : TAS-116; TAS 116;
Codes from synonyms : 75337;
Origin ID : C134448;
UMLS CUI : C5418185;
Currated CISMeF NLP mapping
- TAS-116 [MeSH Supplementary Concept]
- Semantic type(s)
- UMLS correspondences (same concept)
- TAS-116 [MeSH Supplementary Concept]
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
