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Silmitasertib sodium salt

CAS No. : 1309357-15-0

MCE 国际站：Silmitasertib sodium salt

产品活性：Silmitasertib sodium salt 是一种有效、可口服、高度选择性的 CK2 抑制剂，对 CK2α 和 CK2α' 的 IC₅₀值均为 1 nM。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Autophagy

作用靶点：Casein Kinase  |  Autophagy

In Vitro: 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: 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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