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  • Derazantinib

    • ARQ-087;ARQ087;ARQ 087;CPD1093
    货号: abs814655
    CAS号: 1234356-69-4
    分子式: C29H29FN4O
    分子量: 468.57
    产品说明书
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    货号-规格 货期 价格 数量
    abs814655-5mg 1-2周 ¥2591.00
    - +
    abs814655-25mg 1-2周 ¥8214.00
    - +
    大包装询价
    产品描述
    描述

    Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.

    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
    ARQ-087;ARQ087;ARQ 087;CPD1093
    外观
    powder
    可溶性/溶解性
    DMSO :93 mg/mL (198.48 mM)
    生物活性
    靶点
    FGFR2,RET,DDR2,PDGFRβ,PDGFRβ
    In vitro(体外研究)
    ARQ-087 has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein show a positive relationship between ARQ 087 induced G1 cell cycle arrest and subsequent induction of apoptosis. ARQ 087 inhibits the auto-phosphorylation of FGFR1 and FGFR2 in a dose-dependent manner. In Cos-1 cells overexpressing full-length FGFR1, FGFR2, FGFR3 and FGFR4, ARQ 087 inhibits their phosphorylation with EC50 values of < 0.123 μM, 0.185 μM, 0.463 μM, >10 μM respectively. ARQ 087 inhibits FGFR kinase by an ATP competitive mechanism, and is capable of inhibiting both the inactive and fully active forms of the FGFR kinase. Hence, ARQ 087 delays FGFR activation by inhibiting its autophosphorylation, as well as inhibition of the phosphorylated active kinase.
    In vivo(体内研究)
    ARQ 087 attenuates FGFR signaling in SNU-16 human xenograft tumors, leading to a reduction in phospho-FGFR, phospho-FRS2-α, and phospho-ERK, while the total FGFR2 protein is unaffecte. ARQ 087 is effective at inhibiting tumor growth in vivo in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions. ARQ 087 demonstrated efficacy in multiple in vivo xenograft models, and was well tolerated at doses up to 75 mg/kg.
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    • 实验方法 实验条件
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