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  • 3PO
  • 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
  • 货号: abs819061
    CAS号: 18550-98-6;13309-08-5
    分子式: C13H10N2O
    分子量: 210.23
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    货号-规格 货期 价格 数量
    abs819061-5mg 现货 ¥630.00
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    abs819061-25mg 现货 ¥1890.00
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    大包装询价
    产品描述
    描述

    3PO is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.
    基本信息
    别名
    3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
    外观
    white to beige powder
    可溶性/溶解性
    DMSO :42 mg/mL (199.78 mM)

    Ethanol :42 mg/mL (199.78 mM)
    生物活性
    靶点
    PFKFB3
    In vitro(体外研究)
    3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. 3PO can cause G2-M phase arrest.
    In vivo(体内研究)
    i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo[1]. The PK properties of 3PO are examined in C57Bl/6 mice intravenously administered 3PO: clearance CL=2312 mL/min/kg, T1/2=0.3 hr, Cmax=113 ng/ml, AUC0-inf=36 ng/hr/ml. 3PO is reported to have potent activity against a highly relevant mouse model of leukemia.
    参考文献
    参考文献
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