CPI-203

Catalog No.S7304 Batch:S730403

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Technical Data

Formula

C19H18ClN5OS
Molecular Weight 399.90 CAS No. 1446144-04-2
Solubility (25°C)* In vitro DMSO 79 mg/mL (197.54 mM)
Ethanol 5 mg/mL (12.5 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[2]
  • 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.
Animal Study:

[2]
  • Animal Models

    REC-1 tumor-bearing mice

  • Dosages

    2.5 mg/kg twice daily

  • Administration

    i.p

Selleck's CPI-203 has been cited by 15 publications

DELs enable the development of BRET probes for target engagement studies in cells [ Cell Chem Biol, 2023, 30(8):987-998.e24] PubMed: 37490918
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] PubMed: 35758684
Targeting BET proteins BRD2 and BRD3 in combination with PI3K-AKT inhibition as a therapeutic strategy for ovarian clear cell carcinoma [ Mol Cancer Ther, 2021, molcanther.0809.2020] PubMed: 33509905
Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models [ Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831] PubMed: 34045230
A new small-molecule compound, Q308, silences latent HIV-1 provirus by suppressing Tat- and FACT-mediated transcription [ Antimicrob Agents Chemother, 2021, AAC0047021] PubMed: 34491808
Genetically defined syngeneic mouse models of ovarian cancer as tools for the discovery of combination immunotherapy [ Cancer Discov, 2020, CD-20-0818] PubMed: 33158843
ARV-825-induced BRD4 protein degradation as a therapy for thyroid carcinoma. [ Aging (Albany NY), 2020, 12(5):4547-4557] PubMed: 32163373
Vitamin C supplementation expands the therapeutic window of BETi for triple negative breast cancer. [ EBioMedicine, 2019, 43:201-210] PubMed: 30975544
A novel bromodomain inhibitor, CPI-203, serves as an HIV-1 latency-reversing agent by activating positive transcription elongation factor b. [ Biochem Pharmacol, 2019, 164:237-251] PubMed: 30991051
Vitamin C Sensitizes Melanoma to BET Inhibitors. [ Cancer Res, 2018, 78(2):572-583] PubMed: 29180474

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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