AZD5153
Mechanism of action: BRD4/BET bromodomain antagonist
Preclinical pharmacology
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
Additional Information
Molecular Cancer Therapuetics
Journal of Medicinal Chemistry
Clinical Cancer Research
Nature Chemical Biology
Gene information from the NCBi
This compound works on the following genes: