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BPRCX807

Chemical Structure : BPRCX807

CAS No.: 2236595-58-5

BPRCX807 (BPRCX-807)

Catalog No.: PC-49200Not For Human Use, Lab Use Only.

BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.
    BPRCX807 is a clean and specific CXCR4 antagonist, shows no significant activity against other chemokine receptors including 10 CCRs, 7 CXCRs, and 1 CX3CR subtypes.
    BPRCX807 can effectively inhibit CXCL12/CXCR4 axis-mediated migration of HCC cells, reverses the hypoxia-induced EMT in vitro, also alleviates a hypoxia-induced decrease in the epithelial markers (E-cadherin, MTA-3, CLDN3, and CLDN5) in HCA-1 cells.
    BPRCX807 suppresses metastatic progression of hepatocellular carcinoma (HCC), and sensitizes HCC to sorafenib treatment in orthotopic HCC models, inhibits angiogenesis and remodels the immunosuppressive tumor microenvironment in the orthotopic HCA-1 model.
    BPRCX807 demonstrated synergistic effects with immune therapy anti-PD-1 Ab in the orthotopic HCA-1 model.

    Physicochemical Properties

    M.Wt 613.808
    Formula C31H51N9O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (3-(4-((2-(((4-(3-((3-(cyclohexylamino)propyl)amino)propyl)oxazol-2-yl)methyl)amino)-6-methylpyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropyl)glycine

    References

    1. Jen-Shin Song, et al. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2015433118.

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