BET inhibitor CF53

Modify Date: 2024-01-02 17:11:53

BET inhibitor CF53 Structure
BET inhibitor CF53 structure
Common Name BET inhibitor CF53
CAS Number 1808160-52-2 Molecular Weight 443.50
Density N/A Boiling Point N/A
Molecular Formula C24H25N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BET inhibitor CF53


CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, 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, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].

 Names

Name CF53

 BET inhibitor CF53 Biological Activity

Description CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, 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, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].
Related Catalog
Target

BRD4 (BD1):<1 nM (Ki)

BRD4 (BD1):2 nM (IC50)

BRD4 (BD1):2.2 nM (Kd)

BRD4 (BD2):0.8 nM (Kd)

BRD2 (BD2):0.6 nM (Kd)

BRD2 (BD1):1.1 nM (Kd)

BRD3 (BD2):0.49 nM (Kd)

BRD3 (BD1):0.52 nM (Kd)

BRDT (BD2):1 nM (Kd)

BRDT (BD1):2 nM (Kd)

CREBBP:47 nM (Kd)

EP300:110 nM (Kd)

CECR2:570 nM (Kd)

In Vitro CF53 (Compound 28) is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1, very selective over non-BET bromodomain-containing proteins. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively[1]. CF53 exhibits potent anti-tumor activity, with IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively[1].
In Vivo CF53 (25, 50 mg/kg, p.o.) exhibits potent anti-tumor activity both in MDA-MB-231 xenograft tumor model and in RS4;11 model[1].
References

[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.

 Chemical & Physical Properties

Molecular Formula C24H25N7O2
Molecular Weight 443.50
Storage condition 2-8℃
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