Art. -Nr.: HY-112610

CF53

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CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d 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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Reinheit: 99.81%
CAS. Nr.: 1808160-52-2
Formel: C₂₄H₂₅N₇O₂
Molecular Weight:443.50

Speicherung:

-20°C, stored under nitrogen

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

CF53 Chemical Structure

CAS. Nr.: 1808160-52-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	0.4 μM Compound: 6; CF53	Antiproliferative activity against human HEL cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay Antiproliferative activity against human HEL cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay	[PMID: 36622852]
HEL	IC₅₀	0.6 μM Compound: 6; CF53	Antiproliferative activity against human HEL cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human HEL cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 36622852]
HL-60	IC₅₀	1.4 μM Compound: 6; CF53	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay	[PMID: 36622852]
HL-60	IC₅₀	1.5 μM Compound: 6; CF53	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 36622852]
K562	IC₅₀	0.21 nM Compound: 6; CF53	Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay	[PMID: 36622852]
K562	IC₅₀	2.3 μM Compound: 6; CF53	Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 36622852]
MDA-MB-231	IC₅₀	1.6 μM Compound: 6; CF53	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of SAHA by CCK-8 assay	[PMID: 36622852]
MDA-MB-231	IC₅₀	3.8 μM Compound: 6; CF53	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 36622852]
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, K_ds 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.

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.

Chemical Information

CAS. Nr. 1808160-52-2
Appearance Solid
Molecular Weight 443.50
Formel C₂₄H₂₅N₇O₂
Color Off-white to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

CF53

GNE-207

Butyrolactone 3

Procyanidin B3

GS-626510

Menin-MLL inhibitor 20

I-BET567

BAY1238097

Anacardic Acid

TTK21

GNE-781

CTB

GNE-049

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

CF53

GNE-207

Butyrolactone 3

Procyanidin B3

GS-626510

Menin-MLL inhibitor 20

I-BET567

BAY1238097

Anacardic Acid

TTK21

GNE-781

CTB

GNE-049

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CF53 Related Classifications

HY-112610 Related Classifications

Bioz