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    InvivoChem Cat #: V3677
    CAS #: 1675204-51-9Purity ≥98%

    Description: BMS-242 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value in the range of 6-100 nM in cell free assays. It was first discovered by Bristol-Myers Squibb. Blockade of the PD-1/PD-L1 immune checkpoint pathway with monoclonal antibodies has provided significant advances in cancer treatment. The antibody-based immunotherapies carry a number of disadvantages such as the high cost of the antibodies, their limited half-life, and immunogenicity. Development of small-molecule PD-1/PD-L1 inhibitors that could overcome these drawbacks is slow because of the incomplete structural information for this pathway. The first chemical PD-1/PD-L1 inhibitors, BMS-1001 and its analogs, have been recently disclosed by Bristol-Myers Squibb. 

    References:  2017 Jul 13;60(13):5857-5867;  2017 Aug 7;8(42):72167-72181; WO/2015034820 A1

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    Molecular Weight (MW)449.59
    CAS No.1675204-51-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10mM
    Chemical Name (R)-2-((2,6-Dimethoxy-4-((2-methyl-[1,1'-biphenyl]-3-yl)methoxy)benzyl)amino)-3-methylbutan-1-ol
    Synonyms BMS-242; BMS 242; BMS242
    SMILES Code CC(C)[[email protected]@H](NCC1=C(OC)C=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OC)CO

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    In Vitro

    In vitro activity: BMS-1001 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value of 2.25 nM in cell free assays. 

    Kinase Assay: BMS disclosed recently the first nonpeptidic small molecule inhibitors against the PD-1/PD-L1 pathway that showed the activity in a homogeneous time-resolved fluorescence (HTRF) binding assay; however no further data supporting their activity were provided.

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


    Structures and the PD-1/PD-L1 blocking potential of BMS compounds.  2017 Aug 7;8(42):72167-72181.



    Cytotoxicity and activity of BMS compounds in PD-1/PD-L1 checkpoint assay.  2017 Aug 7;8(42):72167-72181.


    BMS compounds restore the sPD-L1-supressed activation of Jurkat T-cells.  2017



    BMS-1166 induces binding cleft opening.  2017 Aug 7;8(42):72167-72181.



    Decomposition of BMS-1166.  2017 Aug 7;8(42):72167-72181.


    he prediction of BMS-1001 and −1166 binding sites on PD-L1 surface.  2017 Aug 7;8(42):72167-72181.


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