Biological Activity
CX-4945 is a potent, selective and oral casein kinase 2 (CK2) inhibitor with a Ki of 0.38 nM.
In Vitro
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 CX-4945 is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling[1]. CX-4945 with bortezomib treatment prevents leukemic cells from engaging a functional UPR in order to buffer the bortezomib-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression[2]. 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[3].
In Vivo
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[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.