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    BI-9564
    BI-9564

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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 #: V2909
    CAS #: 1883429-22-8Purity ≥98%

    Description: BI-9564 is a novel, cell-permeable, noncytotoxic, potent, and selective inhibitor of BRD9 (bromodomain-containing protein) and BRD7 BD (bromodomains) with Kd values of 14.1 and 239 nM, and IC50 values of 75 nM and 3.4 µM for BRD9/7 respectively. Selective inhibitors of bromodomain-containing protein 9 (BRD9) may have therapeutic potential in the treatment of human malignancies and inflammatory diseases. BI-9564 is useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings. BI-9564 (<5 10='' 324='' shows='' no='' activity='' against='' and='' at='' an='' inhibition=''>40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM.

    References: . 2016 May 26; 59(10): 4462–4475;  2016 May 26;59(10):4459-61.


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    Molecular Weight (MW) 353.41
    Formula C20H23N3O3
    CAS No. 1883429-22-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 16 mg/mL (45.27 mM) 
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (8.48 mM) 
    SMILES Code O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13
    Synonyms BI-9564; BI 9564; BI9564


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    In Vitro

    In vitro activity: BI-9564 is a cell-permeable, noncytotoxic, potent, and selective inhibitor of BRD9 (bromodomain-containing protein) and BRD7 BD (bromodomains) with Kd values of 14.1 and 239 nM, and IC50 values of 75 nM and 3.4 µM for BRD9/7 respectively. Selective inhibitors of bromodomain-containing protein 9 (BRD9) may have therapeutic potential in the treatment of human malignancies and inflammatory diseases. BI-9564 is useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings. BI-9564 (<5 10='' 324='' shows='' no='' activity='' against='' and='' at='' an='' inhibition=''>40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM. 


    Kinase Assay: BI-9564 is a cell-permeable, noncytotoxic, potent, and selective inhibitor of BRD9 (bromodomain-containing protein) and BRD7 BD (bromodomains) with Kd values of 14.1 and 239 nM, and IC50 values of 75 nM and 3.4 µM for BRD9/7 respectively. BI-9564 (<5 10='' 324='' shows='' no='' activity='' against='' and='' at='' an='' inhibition=''>40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells.


    Cell Assay:To 750,000 MV-4-11 cells in 250 µl growth medium (in IMDM, 10 % FBS, GlutaMAX, 25 mM HEPES and 0,1% 2-Mercaptoethanol) per well compound is added at the desired concentration from a 10 mM stock solution using the HP D300 Digital Dispenser. After 2 hours of incubation with the compound, cells are collected by centrifugation, washed in ice cold PBS and lysed in 15 µl of cell extraction buffer. After 30 minutes on ice, nucleic acids are disrupted by sonication. cMYC levels are measured using the human c-Myc (Total) ELISA Kit.  

    In VivoBI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML
    Animal model Female CIEA-NOG mice engrafted intravenously with 1×107 EOL-1 AML cells stably expressing luciferase and GFP.
    Formulation & Dosage 0.5% Natrosol. 10 mL/kg. Oral administration
    References . 2016 May 26; 59(10): 4462–4475.  2016 May 26;59(10):4459-61.


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

    BI-9564

     . 2016 May 26; 59(10): 4462–4475.

     BI-9564

    Binding mode of the methylpyridopyrimidinone 3 or dimethylpyridinone 4 scaffold in BRD9 BD (compound 3: PDB code 5F2P; compound 4: PDB code 5F25).. 2016 May 26; 59(10): 4462–4475.

     BI-9564

    (a–c) Binding mode of BRD9 BD inhibitors (a) 11, (b) 1, and (c) 2 [compound 11: PDB code 5F1L; compound 1: . 2016 May 26; 59(10): 4462–4475.

     BI-9564

    ITC analysis of compounds 1 and 2 (T = 293.15 K). 


    BI-9564

    1 and 2 block EOL-1 cell proliferation with EC50’s of 1400 and 800 nM, respectively. . 2016 May 26; 59(10): 4462–4475.

     BI-9564

    FRAP assay using U2OS cells transfected with GFP–BRD9


    BI-9564

    Efficacy and tolerability of BRD9 inhibitor 2 in a xenograft model of human AML. . 2016 May 26; 59(10): 4462–4475.

     BI-9564

    Summary of Properties of 1 and 2. . 2016 May 26; 59(10): 4462–4475.


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