Silmitasertib sodium salt 是一种可口服的高度选择性CK2抑制剂，对 CK2α 和 CK2α' 的IC50值均为 1 nM。

Silmitasertib sodium salt is a potent and orally bioavailable, highly selective inhibitor of CK2(IC50 of 1 nM, CK2α).

Silmitasertib 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[3]. Silmitasertib (CX-4945) resultes in cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand. The antiproliferative activity of Silmitasertib is correlated with expression levels of the CK2α catalytic subunit, attenuation of PI3K/Akt signaling[1]. Silmitasertib 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[2].

Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated. It showed robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models[1].

1309357-15-0

C19H12ClN3NaO2

372.76

CX-4945 sodium salt

H2O:16.67 mg/mL (44.84 mM),Need ultrasonic
DMSO:6 mg/mL (16.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years