CX-4945 sodium salt

• CAT Number: I001180
• CAS Number: 1309357-15-0
• Molecular Formula: C19H11ClN3NaO2
• Molecular Weight: 371.75
• Purity: ≥95%
• Target: CK2
• Solubility: in DMSO > 10 mM
• Storage: Store at -20°C
• IC50: 1 nM

CX-4945 (Silmitasertib) sodium salt(CAT: I001180)is a potent and selective ATP-competitive inhibitor of protein kinase CK2. It binds to the CK2α subunit with high affinity, exhibiting a Ki value of 0.38 nM and an IC50 value of 1 nM for recombinant human CK2α. CK2, also known as casein kinase 2, is a serine/threonine protein kinase involved in various cellular processes, including cell proliferation and survival. By inhibiting CK2 activity, CX-4945 has the potential to modulate CK2-dependent signaling pathways and cellular functions. It has been studied for its therapeutic potential in various diseases, including cancer.

Reference

[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.