PBRM1-BD2-IN-8
Based on 1 Customer Validation
PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 98.05%
- CAS No.: 2819989-75-6
- Formula: C15H13BrN2O
- Molecular Weight:317.18
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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
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Biological Activity
IC50: 0.16 μM (PBRM1-BD2)[1]
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Cell Line
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Type | Value | Description | References |
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| LNCaP | IC50 |
9.3 μM
Compound: 34
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Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth measured after 7 days with compound replacement for every 48 hrs by celltiter-glo assay
Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth measured after 7 days with compound replacement for every 48 hrs by celltiter-glo assay
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[PMID: 36227159] |
PBRM1-BD2-IN-8 (0-100 μM; 48 h) inhibits the growth of PBRM1-dependent prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells
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Concentration:0-100 μM
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Incubation Time:48 hours
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Result:Inhibited the growth of LNCaP cells with IC50 value of about 9 μM.
Chemical Information
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CAS No. 2819989-75-6
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Appearance Solid
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Molecular Weight 317.18
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Formula C15H13BrN2O
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Color Off-white to light yellow
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SMILES
O=C1NC(C2=CC=CC(C)=C2)NC3=C1C(Br)=CC=C3
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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 (315.28 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 (7.88 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.
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 (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 3.1528 mL | 15.7639 mL | 31.5278 mL | 78.8196 mL |
| 5 mM | 0.6306 mL | 3.1528 mL | 6.3056 mL | 15.7639 mL | |
| 10 mM | 0.3153 mL | 1.5764 mL | 3.1528 mL | 7.8820 mL | |
| 15 mM | 0.2102 mL | 1.0509 mL | 2.1019 mL | 5.2546 mL | |
| 20 mM | 0.1576 mL | 0.7882 mL | 1.5764 mL | 3.9410 mL | |
| 25 mM | 0.1261 mL | 0.6306 mL | 1.2611 mL | 3.1528 mL | |
| 30 mM | 0.1051 mL | 0.5255 mL | 1.0509 mL | 2.6273 mL | |
| 40 mM | 0.0788 mL | 0.3941 mL | 0.7882 mL | 1.9705 mL | |
| 50 mM | 0.0631 mL | 0.3153 mL | 0.6306 mL | 1.5764 mL | |
| 60 mM | 0.0525 mL | 0.2627 mL | 0.5255 mL | 1.3137 mL | |
| 80 mM | 0.0394 mL | 0.1970 mL | 0.3941 mL | 0.9852 mL | |
| 100 mM | 0.0315 mL | 0.1576 mL | 0.3153 mL | 0.7882 mL |
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