1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase

CF53 

Cat. No.: HY-112610
Handling Instructions

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.

For research use only. We do not sell to patients.

CF53 Chemical Structure

CF53 Chemical Structure

CAS No. : 1808160-52-2

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  • Biological Activity

  • Technical Information

  • References

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].

IC50 & Target[1]

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2548 mL 11.2740 mL 22.5479 mL
5 mM 0.4510 mL 2.2548 mL 4.5096 mL
10 mM 0.2255 mL 1.1274 mL 2.2548 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

443.50

Formula

C₂₄H₂₅N₇O₂

CAS No.

1808160-52-2

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CF53
Cat. No.:
HY-112610
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CF53

Cat. No.: HY-112610