For research use only.
Molecular Weight(MW): 399.90
CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Selleck's CPI-203 has been cited by 7 publications
Purity & Quality Control
Choose Selective Epigenetic Reader Domain Inhibitors
|Description||CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.|
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.  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. 
|In vivo||BRD4 mediates CTD Ser2 phosphorylation in vivo.  In REC-1 tumor-bearing mice, the combination of lenalidomide with CPI203 (2.5 mg/kg i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis. |
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.
|In vitro||DMSO||79 mg/mL warmed (197.54 mM)|
|Ethanol||5 mg/mL (12.5 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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