Cat. No. Name Size Price Add Cart
KI1391CX-49452 mg$272
CX-49455 mg$512
CX-494550 mg$2672
CX-4945100 mg$3792

Chemical Characteristic

Product NameCX-4945
SynonymsSilmitasertib
CAS No.1009820-21-6
Molecular Weight 349.77
FormulaC19H12ClN3O2
Chemical Name5-[(3-Chlorophenyl)amino]benzo[c]-2,6-naphthyridine-8-carboxylic acid
Smilesc1(nc2c(c3cnccc13)ccc(c2)C(=O)O)Nc1cc(ccc1)Cl
Chemical Structure

Biological activities

CX-4945 is a potent, selective, and ATP-competitive inhibitor of CK2. CX-4945 inhibits isoforms of the CK2 catalytic subunits CK2α and CK2α??with an IC50 of 1 nM, and inhibits recombinant CK2 with an IC50 of 2 nM.[1] CX-4945 also inhibits endogenous CK2 activity in Jurkat cells with an IC50 of 100 nM.[2] CX-4945 effectively reduces CK2 enzymatic activity and exhibits a broad range of anti-proliferative activity in cancer cell lines, and the breast cancer cell lines display the widest range of sensitivity. In models of angiogenesis, CX-4945 inhibits human umbilical vein endothelial cell (HUVEC) migration, tube formation, and blocks CK2- dependent hypoxia-induced HIF-1945; transcription in cancer cells with IC50 of 5.5, 2.0 and 4.0 µM, respectively.[1] CX-4945 exhibits a dose-dependent antitumor activity in a xenograft model of PC3 prostate cancer model and is well tolerated.[3] CX-4945 (75 mg/kg) demonstrates robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 in murine xenograft models.[1]

Protocols

CX-4945 is prepared in DMSO in 5 mM and stored at -70°C.[1]

References

[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, 70 (24): 10288-10298.
[2] Anderes K, et al. Discovery and characterization of CX-4945, a selective orally bioavailable small molecule inhibitor of protein kinase CK2: Phase 1 initiated.
[3] Pierre F, et al. Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer. Mol Cell Biochem. 2011, 356 (1-2): 37-43.

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