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PBRM1-BD2-IN-2

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Catalog No. T60156Cas No. 2819989-57-4

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

PBRM1-BD2-IN-2

PBRM1-BD2-IN-2

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Purity: 99.88%
Catalog No. T60156Cas No. 2819989-57-4
PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$117In StockIn Stock
5 mg$268In StockIn Stock
10 mg$395In StockIn Stock
25 mg$592In StockIn Stock
50 mg$828In StockIn Stock
100 mg$1,130In StockIn Stock
500 mg$2,270-In Stock
1 mL x 10 mM (in DMSO)$258In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.88%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.
In vitro
PBRM1-BD2-IN-2 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibits the growth of a PBRM1-dependent prostate cancer cell line. It exhibits binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B, and SMARCA4 with Kd values of 9.3 μM, 10.1 μM, 18.4 μM, and 69 μM, respectively, and inhibits PBRM1-BD2 with an IC50 of 1.0 μM[1].
Chemical Properties
Molecular Weight311.14
FormulaC14H9Cl2FN2O
Cas No.2819989-57-4
SmilesO=C1C=2C(NC(N1)C3=C(Cl)C=CC=C3F)=CC=CC2Cl
Relative Density.1.433 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (144.63 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2140 mL16.0699 mL32.1399 mL160.6994 mL
5 mM0.6428 mL3.2140 mL6.4280 mL32.1399 mL
10 mM0.3214 mL1.6070 mL3.2140 mL16.0699 mL
20 mM0.1607 mL0.8035 mL1.6070 mL8.0350 mL
50 mM0.0643 mL0.3214 mL0.6428 mL3.2140 mL
100 mM0.0321 mL0.1607 mL0.3214 mL1.6070 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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