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CX-4945 (Silmitasertib) | CK2a kinase inhibitor

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Price:
$159.00
Catalog #:
C2949-2s
Quantity:


Product Description

CX-4945 is an orally-available, ATP-competitive, pyridoquinoline-based inhibitor of CK2a with an IC50 potency of 1 nM and Ki of 0.38 nM. [1, 2] In a panel of 238 kinases at 500 nM, only 7 inhibited CK2 >90% [2] Treatment of BT474 and BxPC-3 cells with CX-4945 led to rapid dephosphorylation of CK2, Akt (S129), accompanied by reduction in phsophorylation at T308 and S473 of Akt. Since no reduction in PTEN phosphorylation at CK2's S370/S380, it is surmised that CX-4945 suppresses Pi3K/Akt signaling by directly blocking phosphorylation of Akt at Akt at S129 by CK2, rather than through activation of PTEN. [2]

Additionally, CX-4945 inhibits hypoxia-driven hypoxia inducible factor (HIF-1a) activity and prevents downregulation of pVHL and p53. CX-4945 also exerts a regulatory effect on the secretion of IL-6 in inflammatory breast cancer. [3]

CX-4945 may also be a potential sensitizer for resistant cells to conventional chemotherapeutic agents such as gemcitabine and cisplatin. [4]


Technical information:

Chemical Formula:   C19H12ClN3O2
CAS #:   1009820-21-6
Molecular Weight:   349.77
Purity:   > 99%
Appearance:   Yellow
Chemical Name:   5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid
Solubility:   Up to 100 mM in DMSO
Synonyms:   CX-4945, CX 4945, CX4945, Silmitasertib

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Pierre 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, 37-43. Pubmed ID: 21755459
2. Siddiqui-Jain 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, 10288-10298. Pubmed ID: 21159648
3. Kim et al., Druggability of the CK2 inhibitor CX-4945 as an anticancer drug and beyond.. Arch. Pharm. Res. 2012, 35(8), 1293-1296. Pubmed ID: 22941473
4. Zanin et al., Effects of the CK2 inhibitors CX-4945 and CX-5011 on drug-resistant cells.. PLosONE, 2012, 7(11), e49193. Pubmed ID: 21159648

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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