PBRM1-BD2-IN-7
PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 2819989-68-7
- Formula: C16H15ClN2O
- Molecular Weight:286.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
Description
IC50 & Target
IC50: 0.29 μM (PBRM1-BD2)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
2 μM
Compound: 26
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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] |
| PC-3 | IC50 |
2 μM
Compound: 26
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Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth measured after 6 days with compound replacement for every 48 hrs by celltiter-glo assay
Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth measured after 6 days with compound replacement for every 48 hrs by celltiter-glo assay
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[PMID: 36227159] |
In Vitro
PBRM1-BD2-IN-7 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line[1].
PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with IC50 value of 0.29 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human prostate cell lines LNCaP, PC3, and RWPE-1
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Concentration:0, 0.1, 1, and 10 μM
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Incubation Time:5 days
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Result:Inhibited LNCaP growth at higher concentrations.
Chemical Information
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CAS No. 2819989-68-7
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Molecular Weight 286.76
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Formula C16H15ClN2O
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SMILES
O=C1NC(C2=C(C)C=CC=C2C)NC3=C1C(Cl)=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (348.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (8.72 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
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4872 mL | 17.4362 mL | 34.8724 mL | 87.1809 mL |
| 5 mM | 0.6974 mL | 3.4872 mL | 6.9745 mL | 17.4362 mL | |
| 10 mM | 0.3487 mL | 1.7436 mL | 3.4872 mL | 8.7181 mL | |
| 15 mM | 0.2325 mL | 1.1624 mL | 2.3248 mL | 5.8121 mL | |
| 20 mM | 0.1744 mL | 0.8718 mL | 1.7436 mL | 4.3590 mL | |
| 25 mM | 0.1395 mL | 0.6974 mL | 1.3949 mL | 3.4872 mL | |
| 30 mM | 0.1162 mL | 0.5812 mL | 1.1624 mL | 2.9060 mL | |
| 40 mM | 0.0872 mL | 0.4359 mL | 0.8718 mL | 2.1795 mL | |
| 50 mM | 0.0697 mL | 0.3487 mL | 0.6974 mL | 1.7436 mL | |
| 60 mM | 0.0581 mL | 0.2906 mL | 0.5812 mL | 1.4530 mL | |
| 80 mM | 0.0436 mL | 0.2180 mL | 0.4359 mL | 1.0898 mL | |
| 100 mM | 0.0349 mL | 0.1744 mL | 0.3487 mL | 0.8718 mL |
PBRM1-BD2-IN-7 Related Classifications
HY-151534 Related Classifications
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