CF53

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].

Product Specifications

CAS Number

[1808160-52-2]

UNSPSC

12352005

Target

Epigenetic Reader Domain; Histone Acetyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CF53.html

Purity

99.81

Solubility

DMSO : 110 mg/mL (ultrasonic)

Smiles

COC1=C(C2=C(C)ON=C2C)C=C(NC3=C4C(NC5=CC(C6CC6)=NN5C)=NC(C)=N3)C4=C1

Molecular Formula

C24H25N7O2

Molecular Weight

443.50

References & Citations

[1]Zhao Y, et al. Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor. J Med Chem. 2018 Jul 26;61 (14) :6110-6120.