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  • Silmitasertib

    • CX-4945;CX 4945;CX4945
    货号: abs810769
    CAS号: 1009820-21-6
    分子式: C19H12ClN3O2
    分子量: 349.77
    产品说明书
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    货号-规格 货期 价格 数量
    abs810769-10mg 1-2周 ¥1300.00
    - +
    abs810769-50mg 1-2周 ¥3900.00
    - +
    大包装询价
    产品描述
    描述

    Silmitasertib is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively.

    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
    CX-4945;CX 4945;CX4945
    外观
    Orange powder
    可溶性/溶解性
    DMSO : ≥ 35 mg/mL (100.07 mM)
    生物活性
    靶点
    CK2
    In vitro(体外研究)
    Silmitasertib (CX-4945) causes cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand, and the antiproliferative activity of Silmitasertib (CX-4945) is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling. Silmitasertib (CX-4945) with PS-341 treatment prevents leukemic cells from engaging a functional UPR in order to buffer the PS-341-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression. Silmitasertib (CX-4945) induces cytotoxicity and apoptosis, and exerts anti-proliferative effects in hematological tumors by downregulating CK2 expression and suppressing activation of CK2-mediated PI3K/Akt/mTOR signaling pathways.
    In vivo(体内研究)
    Silmitasertib (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.
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    • 实验方法 实验条件
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