Preferred Label : Bivalent BRD4 Inhibitor AZD5153;
NCIt synonyms : Bivalent BET Bromodomain Inhibitor AZD5153; BRD4/BET Bromodomain Antagonist AZD5153; (R)-4-(2-(4-(1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one; BET Inhibitor AZD5153;
NCIt related terms : AZD-5153;
NCIt definition : An orally bioavailable bivalent inhibitor of bromodomain-containing protein 4 (BRD4),
with potential antineoplastic activity. Upon oral administration, the BRD4 inhibitor
AZD5153 selectively binds to the acetylated lysine recognition motifs in two bromodomains
in the BRD4 protein, thereby preventing the binding of BRD4 to acetylated lysines
on histones. This disrupts chromatin remodeling and dysregulates expression of target
genes, which leads to the downregulation of the expression of certain growth-promoting
genes, induces apoptosis and inhibits the proliferation of BRD4-overexpressing tumor
cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of
proteins, is a transcriptional regulator that is overexpressed in certain tumor cells
and plays an important role in cellular proliferation.;
UNII : C7C7U6YEAO;
CAS number : 1869912-39-9;
Molecule name : AZD 5153; AZD5153;
NCI Metathesaurus CUI : CL553171;
Origin ID : C151943;
UMLS CUI : C4508067;
Semantic type(s)
- UMLS correspondences (same concept)
- AZD5153 [MeSH Supplementary Concept]
- concept_is_in_subset
- has_target
