2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. 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, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.

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CF53 Chemical Structure

CF53 Chemical Structure

CAS No. : 1808160-52-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 407 In-stock
Solution
10 mM * 1 mL in DMSO USD 407 In-stock
Solid
5 mg USD 370 In-stock
10 mg USD 555 In-stock
50 mg USD 1220 In-stock
100 mg USD 1650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

CF53 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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, 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)

CECR2

570 nM (Kd)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
85 nM
Compound: 28; CF53
Growth inhibition of human MDA-MB-231 cells after 4 days by WST-8 assay
Growth inhibition of human MDA-MB-231 cells after 4 days by WST-8 assay
[PMID: 30015487]
MOLM-13 IC50
7 nM
Compound: 28; CF53
Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay
Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay
[PMID: 30015487]
In Vitro

CF53 (Compound 28) 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 IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CF53 Related Antibodies
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 in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

443.50

Formula

C24H25N7O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (248.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.83 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.83 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.78%

SDS (251 KB)

COA (254 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2548 mL 11.2740 mL 22.5479 mL 56.3698 mL
5 mM 0.4510 mL 2.2548 mL 4.5096 mL 11.2740 mL
10 mM 0.2255 mL 1.1274 mL 2.2548 mL 5.6370 mL
15 mM 0.1503 mL 0.7516 mL 1.5032 mL 3.7580 mL
20 mM 0.1127 mL 0.5637 mL 1.1274 mL 2.8185 mL
25 mM 0.0902 mL 0.4510 mL 0.9019 mL 2.2548 mL
30 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8790 mL
40 mM 0.0564 mL 0.2818 mL 0.5637 mL 1.4092 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1274 mL
60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9395 mL
80 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7046 mL
100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 mL
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CF53 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CF531808160-52-2CF 53CF-53Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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