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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.05%
- CAS 番号: 2819989-75-6
- 分子式: C15H13BrN2O
- 分子量:317.18
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
SWI/SNF Complex アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
IC50: 0.16 μM (PBRM1-BD2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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
|
[PMID: 36227159] |
体外実験
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.
化学情報
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CAS 番号 2819989-75-6
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性状 Solid
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分子量 317.18
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
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.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (254 KB)
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- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
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 |