BET bromodomain-IN-5
Based on 1 Customer Validation
BET bromodomain-IN-5 is an orally active BET inhibitor with an IC50 of 14 nM against BRD4 (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors.
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 1505453-59-7
- Formula: C24H20ClN5O2
- Molecular Weight:445.90
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
BET[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | GI50 |
15 nM
Compound: 44
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Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay
Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay
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[PMID: 26572217] |
BET bromodomain inhibitor (Compound 11) (0.001-10 μM; 4 days) can inhibit the proliferation of KMS-28PE plasmacytoma cells and AMO-1 multiple myeloma cells, and induce cell cycle arrest and apoptosis[1].
BET bromodomain inhibitor (Compound 44) has a GI50 of 15 nM against MV4-11 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1505453-59-7
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Appearance Solid
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Molecular Weight 445.90
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Formula C24H20ClN5O2
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Color White to off-white
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SMILES
O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(C4=CN(C)N=C4)=CC=C3C5=C1ON=C5C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 100 mg/mL (224.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2427 mL | 11.2133 mL | 22.4266 mL | 56.0664 mL |
| 5 mM | 0.4485 mL | 2.2427 mL | 4.4853 mL | 11.2133 mL | |
| 10 mM | 0.2243 mL | 1.1213 mL | 2.2427 mL | 5.6066 mL | |
| 15 mM | 0.1495 mL | 0.7476 mL | 1.4951 mL | 3.7378 mL | |
| 20 mM | 0.1121 mL | 0.5607 mL | 1.1213 mL | 2.8033 mL | |
| 25 mM | 0.0897 mL | 0.4485 mL | 0.8971 mL | 2.2427 mL | |
| 30 mM | 0.0748 mL | 0.3738 mL | 0.7476 mL | 1.8689 mL | |
| 40 mM | 0.0561 mL | 0.2803 mL | 0.5607 mL | 1.4017 mL | |
| 50 mM | 0.0449 mL | 0.2243 mL | 0.4485 mL | 1.1213 mL | |
| 60 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9344 mL | |
| 80 mM | 0.0280 mL | 0.1402 mL | 0.2803 mL | 0.7008 mL | |
| 100 mM | 0.0224 mL | 0.1121 mL | 0.2243 mL | 0.5607 mL |