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CPI203

🥰Excellent
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

🥰Excellent
Purity: 99.71%
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 SizePriceAvailabilityQuantity
5 mg$30In Stock
10 mg$45In Stock
25 mg$72In Stock
50 mg$133In Stock
1 mL x 10 mM (in DMSO)$30In Stock
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Purity:99.71%
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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)
AliasCPI-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.
Solubility Information
DMSO: 200 mM
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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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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