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  • JPH203

    • KYT-0353;JPH-203;JPH 203
    货号: abs818331
    CAS号: 1037592-40-7
    分子式: C23H19Cl2N3O4
    分子量: 472.32
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    货号-规格 货期 价格 数量
    abs818331-5mg 现货 ¥650.00
    - +
    abs818331-25mg 1-2周 ¥1550.00
    - +
    abs818331-100mg 1-2周 ¥3150.00
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    大包装询价
    产品描述
    描述

    JPH203 is a potent and selective L-type amino acid transporter 1 (LAT-1) inhibitor. 

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    KYT-0353;JPH-203;JPH 203
    外观
    light-yellow to off-white solid
    可溶性/溶解性
    0.1N hydrochloric acid : 7.3 mg/mL (15.46 mM; Need ultrasonic and warming)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)
    生物活性
    靶点
    LAT1
    In vitro(体外研究)
    JPH203 is a selective inhibitor of LAT1. JPH203 (KYT-0353) inhibits 14C-leucine uptake in S2-hLAT1 and HT-29 cells, with IC50s of 0.14 μM and 0.06 μM. JPH203 (3-1000 μM) exhibits concentration-dependent inhibitory effects on S2-hLAT1 cell growth with an IC50 of 16.4 μM. JPH203 also displays inhibitory activities against HT-29 cell growth, with an IC50 value of 4.1 μM. JPH203 (0.001-100 μM) inhibits the 14C-leucine (1.0 μM) uptake in a concentration dependent way by the YD-38 cells with an IC50 value of 0.79 ± 0.06 μM. JPH203 slightly shows such effects in normal human oral keratinocytes (NHOKs). JPH203 (0.01-30 mM, 1-4 d) completely inhibits the proliferation of YD-38 cells in a dose- and time-dependent manner. However, JPH203 slightly inhibits the proliferation of NHOKs. JPH203 (30 mM) induces apoptosis of YD-38 cells. JPH203 (3 mM) also increases the level of cleaved PARP in activation of the caspases cascade. JPH203 (30 mM) induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. JPH203 (0.001-100 µM) inhibits 14C-leucine (1.0 µM) uptake slightly in FOB cells with an IC50 value of 92.12 ± 10.71 µM, but potently exihibts such effects in Saos2 cells with an IC50 value of 1.31 ± 0.27 µM. JPH203 (0.01 to 30 mM, 1-4 d) potently inhibits cell proliferation in Saos2 cells in a dose- and time-dependent manner, with an IC50 of 4.09-0.09 mM, but slightly inhibits that of FOB cells, with an IC50 of 24.1-2.8 mM.
    In vivo(体内研究)
    JPH203 (6.3, 12.5, and 25.0 mg/kg, i.v. for 14 days) exhibits dose-dependent inhibition on HT-29 tumor growth in nude mice.
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