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  • GSK1838705A

    货号: abs813286
    CAS号: 1116235-97-2
    分子式: C27H29FN8O3
    分子量: 532.57
    产品说明书
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    货号-规格 货期 价格 数量
    abs813286-5mg 1-2周 ¥1309.00
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    abs813286-10mg 1-2周 ¥2401.00
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    abs813286-25mg 1-2周 ¥4245.00
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    abs813286-50mg 1-2周 ¥7641.00
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    大包装询价
    产品描述
    描述

    GSK1838705A是一种有效的IGF-1R抑制剂,IC50为2.0 nM,适度有效作用于IR和ALK,IC50分别为1.6 nM和0.5 nM,对其他蛋白激酶几乎没有作用活性。

    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 :53.3 mg/mL (100 mM)
    生物活性
    靶点
    ALK ,Insulin Receptor ,IGF-1R
    In vitro(体外研究)
    GSK1838705A potently and ATP-competitively inhibits IGF-1R and IR with appKi values of 0.7 nM and 1.1 nM, respectively.In cells, GSK1838705A potently inhibits ligand-induced phosphorylation of IGF-1R and IR with IC50 of 85 nM and 79 nM, respectively. GSK1838705A shows the significant anti-proliferative effect in a panel of cell lines derived from solid and hematologic tumors such as L-82, SUP-M2, SK-ES and MCF-7 cells with EC50 of 24 nM, 28 nM, 141 nM and 203 nM, respectively. GSK1838705A shows an accumulation of MCF-7 and NCl-H929 cells predominantly in G1 (2N) phase of the cell cycle. GSK1838705A also inhibits ALK with Ki of 0.35 nM and supresses the proliferation of nucleophosmin (NPM)-ALK fusion cells with EC50 of 24-88 nM. GSK1838705A potently inhibits NPM-ALK phosphorylation in Karpas-299 and SR-786 cells, while has modest effect on STAT3 phosphorylation.
    In vivo(体内研究)
    In NIH-3T3/LISN tumor-bearing mice, oral treatment of GSK1838705A (60 mg/kg) cause tumor growth inhibition by 77%, without significant weight loss. In COLO 205 tumor-bearing mice, inhibition of tumor growth by GSK1838705A (30 mg/kg) is 80%. Besides, the antitumor efficacy of GSK1838705A is also observed in mice bearing HT29 xenograft or BxPC3 xenograft. In mice, GSK1838705A (60 mg/kg) leads to a transient 2-fold increase in blood glucose levels by inhibiting IR signaling. GSK1838705A (60 mg/kg) inhibits the growth of established Karpas-299 xenografts with 93% tumor growth inhibition, with no effect on weights of the rats.
    参考文献
    参考文献
    Anaplastic Lymphoma Kinase: role in specific tumours, and development of small molecule inhibitors for cancer therapy.
    Ardini E,et al. Cancer Lett. 2010 Dec 28;299(2):81-94. PMID:
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