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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Ephrin Receptor-UniPR1331
UniPR1331

Chemical Structure : UniPR1331

CAS No.: 1809170-59-9

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UniPR1331 (UniPR-1331)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 560.779
    分子式 C35H48N2O4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

    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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