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  • NVP-AEW541

    货号: abs817724
    CAS号: 475489-16-8
    分子式: C27H29N5O
    分子量: 439.55
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs817724-2mg 1-2周 ¥1274.00
    - +
    abs817724-5mg 1-2周 ¥2202.00
    - +
    abs817724-10mg 1-2周 ¥3129.00
    - +
    abs817724-50mg 1-2周 ¥8448.00
    - +
    大包装询价
    产品描述
    描述
    NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM, greater potency and selectivity for IGF-1R in a cell-based assay.
    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
    可溶性/溶解性
    DMSO:88 mg/mL (200.2 mM)
    生物活性
    靶点
    IGF-1R
    In vitro(体外研究)
    NVP-AEW541 inhibits the in vitro kinase activity of the recombinant IGF-IR kinase domain with an IC50 value of 0.15 μM and to be equipotent against the recombinant InsR kinase domain. NVP-AEW541 is confirmed active toward the IGF-IR kinase (IC50=86 nM) and shown to be selective at the cellular level. Indeed, NVP-AEW541 is found to be 27-fold more potent toward the native IGF-IR, as compared to the structurally related native InsR (IC50=2.3 μM). NVP-AEW541 suppresses the IGF-I-mediated survival, soft agar and proliferation of MCF-7 cells with IC50 of 0.162 μM, 0.105 μM and 1.64 μM, respectively.
    In vivo(体内研究)
    Oral administration of NVP-AEW541 (20, 30, or 50 mg/kg) results in abrogation of basal and IGF-I-induced receptor, and PKB and MAPK phosphorylation in the NWT-21 tumor xenograft. NVP-AEW541 is administered by oral gavage twice a day for 14 consecutive days. The control group is similarly treated with 0.2 mL carrier twice a day. Tumor volume and animal weight are measured thrice a week till the end of the treatment. At that time, animals are sacrificed and tumors are collected and formalin fixed for histologic and immunohistochemical analyses. In both cases, NVP-AEW541 treatment causes tumor shrinkage that reached the statistical significance (P=0.0156 and P=0.0111 for HTLA-230 and SK-N-BE2c, respectively).
    参考文献
    参考文献
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