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  • Afatinib (BIBW2992)

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    • 阿法替尼;Afatinib;BIBW2992;BIBW-2292
    货号: abs810678
    CAS号: 439081-18-2;850140-72-6
    分子式: C24H25ClFN5O3
    分子量: 485.94
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    货号-规格 货期 价格 数量
    abs810678-5mg 现货 ¥781.00 ¥234.00
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    abs810678-50mg 现货 ¥3283.00 ¥985.00
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    产品描述
    描述

    BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively.

    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
    阿法替尼;Afatinib;BIBW2992;BIBW-2292
    外观
    White to off-white powder
    可溶性/溶解性
    DMSO :97 mg/mL (199.61 mM)

    Ethanol :15 mg/mL (30.86 mM)
    生物活性
    靶点
    EGFR (L858R);EGFR (wt);ErbB4;EGFR (L858R/T790M);HER2
    In vitro(体外研究)
    BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatinib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2.
    In vivo(体内研究)
    Daily oral administration of BIBW2992 at 20 mg/kg for 25 days results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Reduced phosphorylation of EGFR and AKT is confirmed by immunohistochemical staining of tissue sections. Therefore, like lapatinib and neratinib, BIBW2992 is a next generation tyrosine kinase inhibitor (TKI) that inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases irreversibly. BIBW2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those insensitive to these standard therapies.
    参考文献
    参考文献
    [1] Li D, et al. Oncogene, 2008, 27(34), 4702-4711.
    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
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