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  • Lapatinib(free base)

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    • GW572016;GW-572016;GW 572016
    货号: abs812860
    CAS号: 231277-92-2
    分子式: C29H26ClFN4O4S
    分子量: 581.06
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    货号-规格 货期 价格 数量
    abs812860-25mg 现货 ¥441.00 ¥132.00
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    abs812860-100mg 现货 ¥807.00 ¥242.00
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    产品描述
    描述

    Lapatinib,以 Lapatinib Ditosylate的形式使用,是一种有效的EGFR和ErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。

    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
    GW572016;GW-572016;GW 572016
    外观
    Powder
    可溶性/溶解性
    DMSO:100 mg/mL (172.09 mM)
    生物活性
    靶点
    ErbB2 ,EGFR ,ErbB4
    In vitro(体外研究)
    Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation.
    In vivo(体内研究)
    Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner.
    参考文献
    参考文献
    [1] Rusnak DW, et al. Mol Cancer Ther, 2001, 1(2), 85-94.
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