BET-IN-14
Based on 1 Customer Validation
BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 has anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 98.87%
- CAS No.: 2243669-93-2
- Formula: C30H37N7O2
- Molecular Weight:527.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
BET (IC50: 5.35 nM)
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Cell Line
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Type | Value | Description | References |
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| MM1.S | IC50 |
26.1 nM
Compound: 14
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Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay
Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay
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[PMID: 31490070] |
BET-IN-14 (Compound 171) (72 h) shows anti-tumor activity against various cancer cell lines (average IC50: 174.7 nM), especially in MM.1S, Ty-82, MV-4-11, and KG-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H522, RKO, NCI-H1299, MM.1S, Ty-82, MV-4-11, and KG-1 cells
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Concentration:0-1 μM approximately
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Incubation Time:72 h
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Result:Showed anti-tumor activity with average IC50 of 174.7 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human MV-4-11 xenografts in Balb/c nude mice[1]
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Dosage:50 and 100 mg/kg
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Administration:p.o., qd
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Result:Inhibited tumor growth by 60.36%.
Chemical Information
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CAS No. 2243669-93-2
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Appearance Solid
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Molecular Weight 527.66
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Formula C30H37N7O2
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Color Light yellow to yellow
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SMILES
CC1=CC=C(N2C(C3=CC(N(C4CCCC4)[C@H](C)C(N5C)=O)=C5C=C3)=NC(C(N6CCN(C)CC6)=O)=N2)C=C1
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (189.52 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: 2.5 mg/mL (4.74 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (4.74 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (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)
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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, 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 | 1.8952 mL | 9.4758 mL | 18.9516 mL | 47.3790 mL |
| 5 mM | 0.3790 mL | 1.8952 mL | 3.7903 mL | 9.4758 mL | |
| 10 mM | 0.1895 mL | 0.9476 mL | 1.8952 mL | 4.7379 mL | |
| 15 mM | 0.1263 mL | 0.6317 mL | 1.2634 mL | 3.1586 mL | |
| 20 mM | 0.0948 mL | 0.4738 mL | 0.9476 mL | 2.3689 mL | |
| 25 mM | 0.0758 mL | 0.3790 mL | 0.7581 mL | 1.8952 mL | |
| 30 mM | 0.0632 mL | 0.3159 mL | 0.6317 mL | 1.5793 mL | |
| 40 mM | 0.0474 mL | 0.2369 mL | 0.4738 mL | 1.1845 mL | |
| 50 mM | 0.0379 mL | 0.1895 mL | 0.3790 mL | 0.9476 mL | |
| 60 mM | 0.0316 mL | 0.1579 mL | 0.3159 mL | 0.7896 mL | |
| 80 mM | 0.0237 mL | 0.1184 mL | 0.2369 mL | 0.5922 mL | |
| 100 mM | 0.0190 mL | 0.0948 mL | 0.1895 mL | 0.4738 mL |