Axitinib
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Axitinib

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    分子式:
    C22H18N4OS
    C22H18N4OS
    分子量:
    386.47
    386.47
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    产品介绍
    产品信息
    抗原名称
    VEGFR1/FLT1 ,VEGFR2/Flk1 ,VEGFR2/KDR ,VEGFR3 ,PDGFRβ
    商品描述

    Axitinib是一种多靶点抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3,PDGFR-β和c-KIT时,其IC50分别为0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM和1.7 nM。Axitinib是受体激酶抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3, PDGFR-β和c-KIT时IC50分别为0.1 , 0.2, 0.1-0.3, 1.6 和1.7 nM 。Axitinib可以阻断VEGFR的自磷酸化作用,VEGF调节的内皮细胞活力,微管形成,及下游信号。Axitinib抑制多种细胞系的增殖,如作用于IGR-N91, IGR-NB8, SH-SY5Y ,无VEGF刺激的HUVEC时IC50分别为>1000 nM, 849 nM, 274 nM和573 nM。

    分子量
    386.47
    纯度

    >98%

    可溶性
    DMSO :9.7 mg/mL (25 mM)
    外观
    类白色粉末
    In vitro(体外研究)
    Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC).
    In vivo(体内研究)
    Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
    背景
    别名
    阿西替尼;AG-013736
    分子式
    C22H18N4OS
    CAS号
    319460-85-0
    制备和贮存
    保存方式
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

    参考图片

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    货号:
    abs813181-1g
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