TRIM24/BRPF1-IN-2
Based on 1 Customer Validation
TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research.
For research use only. We do not sell to patients.
- Purity : 98.67%
- CAS No.: 3033288-68-2
- Formula: C20H22N2O4S
- Molecular Weight:386.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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BRPF1 1.16 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
0.82 μM
Compound: 20l
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Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay
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[PMID: 35385803] |
| LNCaP | IC50 |
1.07 μM
Compound: 20l
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Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay
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[PMID: 35385803] |
| LNCaP C4-2B | IC50 |
0.78 μM
Compound: 20l
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Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay
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[PMID: 35385803] |
In Vitro
TRIM24/BRPF1-IN-2 (compound 20l) (0-10 μM, 48 h) suppresses the growth of the prostate cell lines (C4-2B, LNCaP, and 22Rv1), with IC50 values of 0.78±0.15, 1.07±0.47, and 0.82±0.26 μM, respectively[1].
TRIM24/BRPF1-IN-2 inhibits gene and protein expression in prostate cancer cells[1].
TRIM24/BRPF1-IN-2 displays reasonable Caco-2 permeability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 cell, LNCaP cells
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Concentration:0.4, 2, 5, and 10 μM
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Incubation Time:48 h
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Result:Decreased the mRNA expression of full-length AR, AR-V7 and AR-regulated genes PSA, KLK2 and TMPRSS2. inhibited the mRNA level of C-MYC.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (n = 5-7 per dose group, Four-week-old, male, non-obese diabetic server combined immune-deficiency (NOD SCID), 22Rv1 xenograft model)[1]
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Dosage:50 mg/kg
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Administration:IP, once daily for 21 days
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Result:Inhibited the progression of the tumors significantly (53% tumor growth inhibition) without body weight loss.
Chemical Information
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CAS No. 3033288-68-2
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Appearance Solid
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Molecular Weight 386.46
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Formula C20H22N2O4S
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Color White to off-white
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SMILES
COC1=CC=C(C=C1S(=O)(NC2=CC=C3C(CCN3C(C)=O)=C2)=O)C4CC4
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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
In Vitro:
DMSO : 100 mg/mL (258.76 mM; ultrasonic and warming and heat to 60°C; 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)
In Vivo:
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 (6.47 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.
In Vivo Dissolution Calculator
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 | 2.5876 mL | 12.9379 mL | 25.8759 mL | 64.6897 mL |
| 5 mM | 0.5175 mL | 2.5876 mL | 5.1752 mL | 12.9379 mL | |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5876 mL | 6.4690 mL | |
| 15 mM | 0.1725 mL | 0.8625 mL | 1.7251 mL | 4.3126 mL | |
| 20 mM | 0.1294 mL | 0.6469 mL | 1.2938 mL | 3.2345 mL | |
| 25 mM | 0.1035 mL | 0.5175 mL | 1.0350 mL | 2.5876 mL | |
| 30 mM | 0.0863 mL | 0.4313 mL | 0.8625 mL | 2.1563 mL | |
| 40 mM | 0.0647 mL | 0.3234 mL | 0.6469 mL | 1.6172 mL | |
| 50 mM | 0.0518 mL | 0.2588 mL | 0.5175 mL | 1.2938 mL | |
| 60 mM | 0.0431 mL | 0.2156 mL | 0.4313 mL | 1.0782 mL | |
| 80 mM | 0.0323 mL | 0.1617 mL | 0.3234 mL | 0.8086 mL | |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6469 mL |
TRIM24/BRPF1-IN-2 Related Classifications
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