CF53
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.81%
- CAS No.: 1808160-52-2
- Formule: C24H25N7O2
- Masse moléculaire:443.50
-
Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
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) |
|
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1808160-52-2
-
Appearance Solid
-
Masse moléculaire 443.50
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal 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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
-
Fiche technique (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)
-
Instruction de manipulation (2659 KB)
Références
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 |
CF53 Related Classifications
HY-112610 Related Classifications
Powered by Bioz