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  • CX-4945 sodium salt
    货号: abs819088
    CAS号: 1309357-15-0
    分子式: C19H11ClN3NaO2
    分子量: 371.75
    产品说明书
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    货号-规格 货期 价格 数量
    abs819088-2mg 1-2周 ¥1147.00
    - +
    abs819088-5mg 1-2周 ¥1764.00
    - +
    大包装询价
    产品描述
    描述
    Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
    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
    10 mM in DMSO
    生物活性
    靶点
    Casein Kinase
    In vivo(体内研究)
    CX-4945 (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models.
    参考文献
    参考文献
    [1]. Siddiqui-Jain A et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15;70(24):10288-98.



    [2]. Pierre F et al. Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem. 2011 Jan 27;54(2):635-54.



    [3]. Liu H, Wang X, Wang J, Wang J, Li Y, Yang L, Li G.
    Structural Determinants of CX-4945 Derivatives as Protein Kinase CK2 Inhibitors: A Computational Study.
    Int J Mol Sci. 2011;12(10):7004-21.




    [4]. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM.
    Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
    J Med Chem. 2011 Jan 27;54(2):635-54.




    [5]. Siddiqui-Jain A, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C, Proffitt C, Schwaebe MK, Ryckman DM, Rice WG, Anderes K.
    CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy.
    Cancer Res. 2010 Dec 15;70(24):10288-98.

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