CX4945 (Silmitasertib)

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MedKoo CAT#: 200843

CAS#: 1009820-21-6 (free acid)

Description: Silmitasertib, also know as CX-4945, is an orally bioavailable small-molecule inhibitor of CK2 with potential antineoplastic activity. CK2 inhibitor CX-4945 selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2, a protein kinase often overexpressed in a variety of cancer cell types, appears to be correlated with malignant transformation, tumor growth and survival.

Chemical Structure

CX4945 (Silmitasertib)
CAS# 1009820-21-6 (free acid)

Theoretical Analysis

MedKoo Cat#: 200843
Name: CX4945 (Silmitasertib)
CAS#: 1009820-21-6 (free acid)
Chemical Formula: C19H12ClN3O2
Exact Mass: 349.0618
Molecular Weight: 349.77
Elemental Analysis: C, 65.24; H, 3.46; Cl, 10.14; N, 12.01; O, 9.15

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same day
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1150.0 Same day
1.0g USD 1950.0 Same day
2.0g USD 3250.0 Same day
5.0g USD 5250.0 Same day
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Related CAS #: 1009820-21-6 (free acid)   1309357-15-0 (sodium)    

Synonym: CX4945 CX-4945; CX 4945; Silmitasertib.

IUPAC/Chemical Name: 5-((3-chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid


InChi Code: InChI=1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25)

SMILES Code: O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO (up to 15mg/mL)

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 349.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Son YH, Moon SH, Kim J. The protein kinase 2 inhibitor CX-4945 regulates osteoclast and osteoblast differentiation In vitro. Mol Cells. 2013 Nov;36(5):417-23. doi: 10.1007/s10059-013-0184-9. Epub 2013 Oct 22. PubMed PMID: 24293011.

2: Quotti Tubi L, Gurrieri C, Brancalion A, Bonaldi L, Bertorelle R, Manni S, Pavan L, Lessi F, Zambello R, Trentin L, Adami F, Ruzzene M, Pinna LA, Semenzato G, Piazza F. Inhibition of protein kinase CK2 with the clinical-grade small ATP-competitive compound CX-4945 or by RNA interference unveils its role in acute myeloid leukemia cell survival, p53-dependent apoptosis and daunorubicin-induced cytotoxicity. J Hematol Oncol. 2013 Oct 12;6(1):78. doi: 10.1186/1756-8722-6-78. PubMed PMID: 24283803; PubMed Central PMCID: PMC3852751.

3: Buontempo F, Orsini E, Martins LR, Antunes I, Lonetti A, Chiarini F, Tabellini G, Evangelisti C, Evangelisti C, Melchionda F, Pession A, Bertaina A, Locatelli F, McCubrey JA, Cappellini A, Barata JT, Martelli AM. Cytotoxic activity of the casein kinase 2 inhibitor CX-4945 against T-cell acute lymphoblastic leukemia: targeting the unfolded protein response signaling. Leukemia. 2013 Nov 20. doi: 10.1038/leu.2013.349. [Epub ahead of print] PubMed PMID: 24253024.

4: Kim J, Hwan Kim S. CK2 inhibitor CX-4945 blocks TGF-β1-induced epithelial-to-mesenchymal transition in A549 human lung adenocarcinoma cells. PLoS One. 2013 Sep 4;8(9):e74342. doi: 10.1371/journal.pone.0074342. PubMed PMID: 24023938; PubMed Central PMCID: PMC3762800.

5: Martins LR, Lúcio P, Melão A, Antunes I, Cardoso BA, Stansfield R, Bertilaccio MT, Ghia P, Drygin D, Silva MG, Barata JT. Activity of the clinical-stage CK2-specific inhibitor CX-4945 against chronic lymphocytic leukemia. Leukemia. 2013 Aug 8. doi: 10.1038/leu.2013.232. [Epub ahead of print] PubMed PMID: 23925046.

6: Prins RC, Burke RT, Tyner JW, Druker BJ, Loriaux MM, Spurgeon SE. CX-4945, a selective inhibitor of casein kinase-2 (CK2), exhibits anti-tumor activity in hematologic malignancies including enhanced activity in chronic lymphocytic leukemia when combined with fludarabine and inhibitors of the B-cell receptor pathway. Leukemia. 2013 Oct;27(10):2094-6. doi: 10.1038/leu.2013.228. Epub 2013 Jul 31. PubMed PMID: 23900138.

7: Son YH, Song JS, Kim SH, Kim J. Pharmacokinetic characterization of CK2 inhibitor CX-4945. Arch Pharm Res. 2013 Jul;36(7):840-5. doi: 10.1007/s12272-013-0103-9. Epub 2013 Mar 31. PubMed PMID: 23543629.

8: Zanin S, Borgo C, Girardi C, O'Brien SE, Miyata Y, Pinna LA, Donella-Deana A, Ruzzene M. Effects of the CK2 inhibitors CX-4945 and CX-5011 on drug-resistant cells. PLoS One. 2012;7(11):e49193. doi: 10.1371/journal.pone.0049193. Epub 2012 Nov 8. PubMed PMID: 23145120; PubMed Central PMCID: PMC3493520.

9: Kim J, Kim SH. Druggability of the CK2 inhibitor CX-4945 as an anticancer drug and beyond. Arch Pharm Res. 2012 Aug;35(8):1293-6. doi: 10.1007/s12272-012-0800-9. PubMed PMID: 22941473.

10: Siddiqui-Jain A, Bliesath J, Macalino D, Omori M, Huser N, Streiner N, Ho CB, Anderes K, Proffitt C, O'Brien SE, Lim JK, Von Hoff DD, Ryckman DM, Rice WG, Drygin D. CK2 inhibitor CX-4945 suppresses DNA repair response triggered by DNA-targeted anticancer drugs and augments efficacy: mechanistic rationale for drug combination therapy. Mol Cancer Ther. 2012 Apr;11(4):994-1005. doi: 10.1158/1535-7163.MCT-11-0613. Epub 2012 Jan 20. PubMed PMID: 22267551.

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