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UniPR1331

Chemical Structure : UniPR1331

CAS No.: 1809170-59-9

UniPR1331 (UniPR-1331)

Catalog No.: PC-35435Not For Human Use, Lab Use Only.

UniPR1331 (UniPR-1331) is a selective, orally available antagonist of Eph/ephrin interaction with pIC50 of 5.45, IC50 of 2.9 uM.

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    Biological Activity

    UniPR1331 (UniPR-1331) is a selective, orally available antagonist of Eph/ephrin interaction with pIC50 of 5.45, IC50 of 2.9 uM.
    UniPR1331 demonstrates anti-angiogenic agent in endothelial cells, bioavailable in mice by the oral route and devoid of biological activity on G protein-coupled and nuclear receptors targeted by bile acid derivatives.
    UniPR1331 blocks the tube formation of HBMVEC in a concentration-dependent manner with IC50 of 3.9 uM, dramatically inhibits vessel formation induced by VEGF165 in in vivo in the CAM assay, does not interfere with the kinase activity of VEGFR2.
    UniPR1331 inhibits ephrin-A1 induced EphA2 phosphorylation decreasing EphA2 expression on U87MG cells, without interfering with the enzymatic activity of EphA2.
    UniPR1331 prolongs survival in glioblastoma and potentiates the effect of antiangiogenic therapy in mice.

    Physicochemical Properties

    M.Wt 560.779
    Formula C35H48N2O4
    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

    ((R)-4-((3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoyl)-L-tryptophan

    References

    1. Festuccia C, et al. Oncotarget. 2018 May 11;9(36):24347-24363.

    2. Castelli R, et al. Eur J Med Chem. 2015 Oct 20;103:312-24.

    3. Vivo V, et al. Shock. 2017 Dec;48(6):681-689.

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