Mechanism of action: BRD4/BET bromodomain antagonist
AZD5153 is a bivalent BRD4/BET bromodomain inhibitor with a cellular target engagement IC50 of 1.7nM monitoring BRD4 displacement from super-enhancers and IC50~ 5nM in modulating BRD4 target genes such as MYC and CCR2.
AZD5153 exhibits potent growth inhibition activity (< 100 nM) in majority of hematologic tumor cell lines and ~50% of solid tumor cell lines with diverse tumors’ tissue of origin.
AZD5153 monotherapy shows significant anti-cancer activity in hematologic and solid tumor xenograft models in vivo.
AZD5153 combination therapies demonstrated synergistic anti-cancer activity with select SOCs and targeted agents in vitro and in vivo
Suitable for and exclusions
Restricted to preclinical oncology studies (proposals) only