首页 产品中心
  • Mubritinib (TAK 165)

    • 木利替尼;TAK-165;TAK 165
    货号: abs812035
    CAS号: 366017-09-6
    分子式: C25H23F3N4O2
    分子量: 468.47
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs812035-10mg 现货 ¥607.00
    - +
    abs812035-25mg 现货 ¥1200.00
    - +
    abs812035-200mg 1-2周 ¥4767.00
    - +
    大包装询价
    产品描述
    描述

    Mubritinib (TAK 165)是一种有效的HER2/ErbB2抑制剂,在BT-474细胞中IC50为6 nM;而在BT-474细胞系中对EGFR,FGFR,PDGFR,JAK1,Src和Blk没有抑制作用。

    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
    木利替尼;TAK-165;TAK 165
    外观
    White Powder
    可溶性/溶解性
    DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)
    生物活性
    靶点
    HER2/ErbB2
    In vitro(体外研究)
    Mubritinib displays > 4000-fold selectivity over other tyrosine kinases, such as EGFR, FGFR, PDGFR, Jak1, Src and Blk. Mubritinib even at low concentration of 0.1 μM significantly blocks HER2 phosphorylation, leading to the downregulation of PI3K-Akt and MAPK pathway in cell line BT474 with high level of HER2. Mubritinib not only exhibits highly potent antiproliferative effect in ErbB2-overexpressing cancer cell line BT474 with an IC50 of 5 nM, but also displays marked antiproliferative effects in cell lines with HER2 expressed weakly with IC50 of 53 nM, 90 nM and 91 nM for LNCaP, LN-REC4 and T24, respectively. Mubritinib displays no inhibitory activities against PC-3 cells with HER2 expressed very faintly with IC50 of 4.62 μM, as well as EGFR-overexpressing HT1376 and ACHN cell lines with IC50 of >25 μM.
    In vivo(体内研究)
    Mubritinib significantly inhibits LN-REC4 xenograft with treatment/control tumor volume ratio of 26.5%. Although ineffective to inhibit the growth of UMUC-3 and ACHN cells in vitro (IC50s of 1.812 and >25 μM, respectively), oral administration of Mubritinib (10 or 20 mg/kg per day) significantly inhibits the growth of UMUC-3 and ACHN xenografts with treatment/control tumor volume ratio of 22.9% and 26%, respectively, as compared with Herceptin (20 mg/kg) which is ineffective to UMUC-3 tumor growth.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
      0 张,还能上传 8 提交
          提示: 尊敬的客户您好,如果您对我们的产品有什么疑问或想要了解的,可以点击“我要咨询”按钮填写您的疑问。
          提交不成功?请联系info@absin.cn。
          我要咨询

      促销资讯 更多

        订购信息
        您可以从我们的授权经销商处购买absin产品或获得技术支持。若要查看您所在地区的经销商,请从以下的下拉列表中选择。
        GO
        • 0