CBP/p300-IN-20
Based on 1 Customer Validation
CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 2999742-92-4
- Formula: C22H19ClF3N5O2
- Molecular Weight:477.87
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
CBP/p300 10.1 (pIC50) |
CBP/p300-IN-20 (compound 28) decreases Myc protein in cell-based cMyc HTRF assay, with a pEC50 of 8.5[1].
CBP/p300-IN-20 (1 μM) shows 97% inhibition for p300 and 80% inhibition for CPB[1].
CBP/p300-IN-20 (0.3-1000 nM; 2 h) decreases H3K18 and H3K27 acetylation without affecting H3K9 acetylation and total H3 in COLO 320HSR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:COLO 320HSR cells
-
Concentration:0.3, 1, 3, 10, 30, 100, 300, 1000 nM
-
Incubation Time:2 hours
-
Result:Caused a rapid concentration-dependent decrease in H3K18 and H3K27 acetylation without affecting H3K9 acetylation and total H3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2999742-92-4
-
Appearance Solid
-
Molecular Weight 477.87
-
Formula C22H19ClF3N5O2
-
Color White to off-white
-
SMILES
O=C([C@@H]1N(C(C2(CC(F)(F)C2)C3=CC=C(Cl)C=C3)=O)C[C@H](F)C1)NC4=CC=C5NN=CC5=N4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 200 mg/mL (418.52 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. 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. 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: ≥ 5 mg/mL (10.46 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.46 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 2.0926 mL | 10.4631 mL | 20.9262 mL | 52.3155 mL |
| 5 mM | 0.4185 mL | 2.0926 mL | 4.1852 mL | 10.4631 mL | |
| 10 mM | 0.2093 mL | 1.0463 mL | 2.0926 mL | 5.2315 mL | |
| 15 mM | 0.1395 mL | 0.6975 mL | 1.3951 mL | 3.4877 mL | |
| 20 mM | 0.1046 mL | 0.5232 mL | 1.0463 mL | 2.6158 mL | |
| 25 mM | 0.0837 mL | 0.4185 mL | 0.8370 mL | 2.0926 mL | |
| 30 mM | 0.0698 mL | 0.3488 mL | 0.6975 mL | 1.7438 mL | |
| 40 mM | 0.0523 mL | 0.2616 mL | 0.5232 mL | 1.3079 mL | |
| 50 mM | 0.0419 mL | 0.2093 mL | 0.4185 mL | 1.0463 mL | |
| 60 mM | 0.0349 mL | 0.1744 mL | 0.3488 mL | 0.8719 mL | |
| 80 mM | 0.0262 mL | 0.1308 mL | 0.2616 mL | 0.6539 mL | |
| 100 mM | 0.0209 mL | 0.1046 mL | 0.2093 mL | 0.5232 mL |