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  • Flumatinib (HHGV678)
    Flumatinib (HHGV678)的可视化放大

    Flumatinib (HHGV678)

    A Bcr-Abl inhibitor

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    Flumatinib (HHGV678)的二维码
    • 库存: 现货
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    • 包装
      价格
      促销价
      数量
    • 5mg
      ¥750.00
      600.00
      - +
    • 10mg
      ¥975.00
      780.00
      - +
    • 50mg
      ¥2037.00
      1630.00
      - +
    已选 0 0
    金额: ¥0.00
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    • 货号: ajce49976
    • CAS: 895519-90-1
    • 别名: 4-[(4-甲基-1-哌嗪基)甲基]-N-[6-甲基-5-[[4-(3-吡啶基)-2-嘧啶基]氨基]-3-吡啶基]-3-(三氟甲基)苯甲酰胺,HHGV678
    • 分子式: C29H29F3N8O
    • 分子量: 562.59
    • 纯度: >98%
    • 溶解度: DMSO : ≥ 32 mg/mL (56.88 mM)
    • 储存: Store at -20°C
    • 库存: 现货

    Background

    Flumatinib is an inhibitor of the non-receptor tyrosine kinase Bcr-Abl (IC50 = 1.2 nM).1 It is selective for Bcr-Abl over VEGFR2, c-Src, EGFR, and HER2 at 1 ?M but does inhibit PDGFRβ and c-Kit (IC50s = 307.6 and 665.5 nM, respectively). Flumatinib inhibits the proliferation of K562 chronic myelogenous leukemia (CML) cells expressing wild-type Bcr-Abl (IC50 = 5.1 nM) and 32D cells expressing the Bcr-Abl mutations Bcr-AblQ252H, Bcr-AblY253F, Bcr-AblE255K, Bcr-AblM351T, and Bcr-AblH396P (IC50s = 76.3, 40.4, 123.2, 20.2, and 34.6 nM, respectively), which confer resistance to the c-Abl, Bcr-Abl, PDGFR, and c-Kit inhibitor imatinib . It also induces tumor regression and increases survival time in a K562 mouse xenograft model when administered at a dose of 75 mg/kg per day. Flumatinib also increases the viability of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50 = 1.6 ?M) and reduces the levels of SARS-CoV-2 in the supernatant of Vero E6 infected cells.2


    1.Luo, H., Quan, H., Xie, C., et al.HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistanceLeukemia24(10)1807-1809(2010) 2.Singh, A., and Arkin, I.T.Targeting viral ion channels: A promising strategy to curb SARS-CoV-2Pharmaceuticals (Basel)15(4)396(2022)

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