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  • Bosutinib(SKI-606)

    • 伯舒替尼;SKI-606
    货号: abs810370
    CAS号: 380843-75-4
    分子式: C26H29Cl2N5O3
    分子量: 530.45
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810370-5mg 1-2周 ¥497.00
    - +
    abs810370-10mg 1-2周 ¥546.00
    - +
    abs810370-50mg 1-2周 ¥726.00
    - +
    abs810370-100mg 1-2周 ¥939.00
    - +
    大包装询价
    产品描述
    描述

    Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity.

    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
    伯舒替尼;SKI-606
    外观
    白色粉末
    可溶性/溶解性

    DMSO : 53.1 mg/mL (100 mM)

    Ethanol : 13.3 mg/mL (25 mM)




    生物活性
    靶点
    Abl ,Src
    In vitro(体外研究)
    Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin.
    In vivo(体内研究)
    Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts.
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    • 实验方法 实验条件
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