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CPI203

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Catalog No. T2442Cas No. 202591-23-9
Alias CPI-203, CPI 203

CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).

CPI203

CPI203

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Purity: 99.77%
Catalog No. T2442Alias CPI-203, CPI 203Cas No. 202591-23-9
CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$30In StockIn Stock
10 mg$45In StockIn Stock
25 mg$72In StockIn Stock
50 mg$133-In Stock
1 mL x 10 mM (in DMSO)$30In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.77%
Color:White
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Product Introduction

Bioactivity
Description
CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
Targets&IC50
BET BD:37 nM
In vitro
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. [1] CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. [2]
Kinase Assay
BRD4 α-screen assay: The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor.
Cell Research
MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI <1. (Only for Reference)
SynonymsCPI-203, CPI 203
Chemical Properties
Molecular Weight399.9
FormulaC19H18ClN5OS
Cas No.202591-23-9
SmilesCC=1C2=C(N3C(C(CC(N)=O)N=C2C4=CC=C(Cl)C=C4)=NN=C3C)SC1C
Relative Density.1.51 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: 200 mM, Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5006 mL12.5031 mL25.0063 mL125.0313 mL
5 mM0.5001 mL2.5006 mL5.0013 mL25.0063 mL
10 mM0.2501 mL1.2503 mL2.5006 mL12.5031 mL
20 mM0.1250 mL0.6252 mL1.2503 mL6.2516 mL
50 mM0.0500 mL0.2501 mL0.5001 mL2.5006 mL
100 mM0.0250 mL0.1250 mL0.2501 mL1.2503 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

You can also refer to dose conversion for different animals. More Dose Conversion

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

Keywords

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