CPI-203

Catalog No.S7304

CPI-203 Chemical Structure

Molecular Weight(MW): 399.90

CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.

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Biological Activity

Description CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Targets
IL-6 [1]
(Cell-based assay)
BRD4 [1]
(Cell-free assay)
MYC [1]
(Cell-based assay)
30 nM 37 nM 99 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]

In vivo BRD4 mediates CTD Ser2 phosphorylation in vivo. [1] 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. [2]

Protocol

Kinase Assay:

[1]

+ Expand

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:

[2]

+ Expand
  • Cell lines: 2 PBMC cultures from healthy donors and 9 MCL cell lines (Granta-519, JVM-2, UPN1, Z-138, JeKo-1, ZBR, JBR, Mino, REC-1 cells)
  • Concentrations: 10 μM
  • Incubation Time: 72 hours
  • Method:

    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)
Animal Research:

[2]

+ Expand
  • Animal Models: REC-1 tumor-bearing mice
  • Formulation: --
  • Dosages: 2.5 mg/kg twice daily
  • Administration: i.p
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL warmed (197.54 mM)
Ethanol 5 mg/mL (12.5 mM)
Water Insoluble

* 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.

Chemical Information

Molecular Weight 399.90
Formula

C19H18ClN5OS

CAS No. 1446144-04-2
Storage powder
Synonyms N/A

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID