CAS No. : 1009820-21-6

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000112
Synonyms:5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid
Molecular Formula:C₁₉H₁₂ClN₃O₂
Molecular Weight:349.77
IC50:1 nM
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Appearance:Yellow solid powder
Purity: > 98%
Cat No:I000112
Cas No:1009820-21-6

CX-4945 (Silmitasertib) is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively.
IC50 value: 1 nM
Target: CK2α
in vitro: CX-4945 (CX 4945;Silmitasertib) has broad spectrum anti-proliferative activity in multiple cancer cell lines. CX-4945 is selective for CK2, as it only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 μM, which is 500-fold greater than the IC50 of CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, CX-4945 treatment at 10 μM is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays. CX-4945 exhibits a broad spectrum of antiproliferative activity, and the breast cancer cell lines displays the widest range of sensitivity to CX-4945 with EC50 of 1.71-20.01 μM. The antiproliferative activity of CX-4945 correlates with CK2α mRNA and protein levels but not the CK2α/' catalytic subunit, the regulatory CK2β subunit, and the PI3K/Akt or PTEN mutational status. CX-4945 inhibits PI3K/Akt signaling by directly blocking the phosphorylation of Akt at Serine 129 by CK2 rather than through activation of PTEN. CX-4945 treatment causes reduced phosphorylation of p21 (T145), increased levels of total p21 and p27, and induction of caspase 3/7 activity. CX-4945 treatment induces a G2/M cell-cycle arrest in BT-474 cells and a G1 arrest in BxPC-3 cells.
in vivo: In PC3 xenograft model, administration of CX-4945 at 25 mg/kg, 50 mg/kg, or 75 mg/kg causes tumor growth inhibition with TGI of 19%, 40%, and 86%, respectively. Oral administration of CX-4945 at 25 mg/kg or 75 mg/kg twice daily displays potent antitumor activity in the BT-474 model, with TGI of 88% and 97%, respectively, and 2 of 9 animals in each group showing more than 50% reduction in tumor size compared with the initial tumor volume. In the BxPC-3 model, CX-4945 treatment at 75 mg/kg twice daily shows 93% TGI with 3 animals having no evidence of tumor remaining at the end of the treatment period.

1:CX-4945: the protein kinase CK2 inhibitor and anti-cancer drug shows anti-fungal activity. Masłyk M, Janeczko M, Martyna A, Kubiński K.Mol Cell Biochem. 2017 May 13. doi: 10.1007/s11010-017-3068-z. [Epub ahead of print] PMID: 28501934
2:CX-4945, a selective inhibitor of casein kinase 2, synergizes with B cell receptor signaling inhibitors in inducing diffuse large B cell lymphoma cell death. Mandato E, Nunes SC, Zaffino F, Casellato A, Macaccaro P, Tubi LQ, Visentin A, Trentin L, Semenzato G, Piazza F.Curr Cancer Drug Targets. 2017 Apr 26. doi: 10.2174/1568009617666170427110450. [Epub ahead of print] PMID: 28460620
3:Targeting Protein Kinase CK2: Evaluating CX-4945 Potential for GL261 Glioblastoma Therapy in Immunocompetent Mice. Ferrer-Font L, Villamañan L, Arias-Ramos N, Vilardell J, Plana M, Ruzzene M, Pinna LA, Itarte E, Arús C, Candiota AP.Pharmaceuticals (Basel). 2017 Feb 12;10(1). pii: E24. doi: 10.3390/ph10010024. PMID: 28208677 Free PMC Article
4:Autophagy Induced by CX-4945, a Casein Kinase 2 Inhibitor, Enhances Apoptosis in Pancreatic Cancer Cell Lines. Hwang DW, So KS, Kim SC, Park KM, Lee YJ, Kim SW, Choi CM, Rho JK, Choi YJ, Lee JC.Pancreas. 2017 Apr;46(4):575-581. doi: 10.1097/MPA.0000000000000780. PMID: 28196025
5:CK2 inhibitor CX-4945 destabilizes NOTCH1 and synergizes with JQ1 against human T-acute lymphoblastic leukemic cells. Lian H, Li D, Zhou Y, Landesman-Bollag E, Zhang G, Anderson NM, Tang KC, Roderick JE, Kelliher MA, Seldin DC, Fu H, Feng H.Haematologica. 2017 Jan;102(1):e17-e21. doi: 10.3324/haematol.2016.154013. Epub 2016 Oct 6. No abstract available. PMID: 27758824 Free PMC Article
6:Synergistic cytotoxic effects of bortezomib and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Buontempo F, Orsini E, Lonetti A, Cappellini A, Chiarini F, Evangelisti C, Evangelisti C, Melchionda F, Pession A, Bertaina A, Locatelli F, Bertacchini J, Neri LM, McCubrey JA, Martelli AM.Oncotarget. 2016 Jan 12;7(2):1323-40. doi: 10.18632/oncotarget.6361. PMID: 26593250 Free PMC Article
7:Different Persistence of the Cellular Effects Promoted by Protein Kinase CK2 Inhibitors CX-4945 and TDB. Girardi C, Ottaviani D, Pinna LA, Ruzzene M.Biomed Res Int. 2015;2015:185736. doi: 10.1155/2015/185736. Epub 2015 Oct 19. PMID: 26558259 Free PMC Article
8:Micropillar arrays as potential drug screens: Inhibition of micropillar-mediated activation of the FAK-Src-paxillin signaling pathway by the CK2 inhibitor CX-4945. Kim J, Choi WJ, Moon SH, Jung J, Park JK, Kim SH, Lee JO.Acta Biomater. 2015 Nov;27:13-20. doi: 10.1016/j.actbio.2015.08.041. Epub 2015 Aug 28. PMID: 26318800
9:The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Chon HJ, Bae KJ, Lee Y, Kim J.Front Pharmacol. 2015 Mar 31;6:70. doi: 10.3389/fphar.2015.00070. eCollection 2015. PMID: 25873900 Free PMC Article
10:MEK inhibitor PD-0325901 overcomes resistance to CK2 inhibitor CX-4945 and exhibits anti-tumor activity in head and neck cancer. Bian Y, Han J, Kannabiran V, Mohan S, Cheng H, Friedman J, Zhang L, VanWaes C, Chen Z.Int J Biol Sci. 2015 Feb 23;11(4):411-22. doi: 10.7150/ijbs.10745. eCollection 2015. PMID: 25798061 Free PMC Article
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