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    BMS-1001
    BMS-1001

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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 #: V3674
    CAS #: 113650-03-4 Purity ≥98%

    Description: 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. 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

    Related CAS#: 2113650-04-5 (HCl)  

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    Molecular Weight (MW) 594.66
    Formula C35H34N2O7
    CAS No. 2113650-04-5 (HCl); 2113650-03-4 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10mM
    Water:  N/A
    Ethanol: N/A
    Chemical Name (2-((3-Cyanobenzyl)oxy)-4-((3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-methylbenzyl)oxy)-5-methylbenzyl)-D-serine
    SynonymsBMS-1001 free base; BMS-1001;BMS 1001; BMS1001
    SMILES CodeOC[[email protected]](C(O)=O)NCC1=CC(C)=C(OCC2=CC=CC(C3=CC=C4OCCOC4=C3)=C2C)C=C1OCC5=CC=CC (C#N)=C5.


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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.


    Cell Assay: BMS-1001 presents low toxicity towards tested cell lines and block the interaction of soluble PD-L1 with the cell surface-expressed PD-1. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes

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    ReferencesOncotarget. 2017 Aug 7;8(42):72167-72181.


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

    BMS-242

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

     

    BMS-242

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

     

    BMS-242


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

     

    BMS-242

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

     

    BMS-242

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

     

    BMS-242


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


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