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    CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146)
    CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0424
    CAS #: 1446144-04-2Purity ≥98%

    Description: CPI-203 (RO6870810, JQ-2, TEN010, RG6146) is a novel, selective, cell permeable and orally bioavailable BET bromodomain inhibitor with anticancer activity. It inhibits BRD4 with an IC50 of 37 nM in a BRD4 α-screen assay. CPI 203 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. CPI203 can enhance the antiproliferative effects of rapamycin on human neuroendocrine tumors. CPI203 can downregulate Myc expression, causes G1 cell cycle arrest and attenuate cell proliferation in human pancreatic neuroendocrine tumors. CPI203 arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). 

    References: Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32; Leukemia. 2014 Oct;28(10):2049-59. 

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    Molecular Weight (MW)399.90
    FormulaC19H18ClN5OS
    CAS No.1446144-04-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 79 mg/mL (197.54mM)
    Water: <1 mg/mL
    Ethanol: 5 mg/mL (12.5 mM) 
    Solubility (In vivo)O=C(N)C[[email protected]]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
    SynonymsRO-6870810; CPI203; CPI-203; CPI 203;RO 6870810; TEN010; RG 6146; RG-6146; TEN 010; TEN010; JQ-2; JQ 2; JQ2;  RG-6146; RO6870810; 


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    In Vitro

    In vitro activity: 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


    Kinase 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: MCL primary cells and 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)) 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.

    In VivoBRD4 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
    Animal modelTreatment with JQ1 derivative CPI203 inhibits BRD4 phosphorylation of CTD Ser2 in vivo. HeLa cells were transfected as above and treated with increasing concentrations of CPI203.
    Formulation & Dosage2.5 mg/kg i.p.
    References Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    CPI-203

    BRD4 phosphorylates CTD Ser2 in vivo. Proc Natl Acad Sci U S A. 2012 May 1; 109(18): 6927–6932.

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