CX-4945

Tocris Bioscience | Catalog # 8993

Potent and selective CK2α and CK2α' inhibitor. Also blocks CK2-dependent HIF-1α transcription, causes cell-cycle arrest, induces apoptosis in cancer cells and induces stem cell reprogramming
Tocris Bioscience
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Key Product Details

Description

Potent and selective CK2α and CK2α' inhibitor. Also blocks CK2-dependent HIF-1α transcription, causes cell-cycle arrest, induces apoptosis in cancer cells and induces stem cell reprogramming

Alternative Names

Silmitasertib

Product Description

CX-4945 (Silmitasertib) is a potent and selective inhibitor of protein kinase CK2α and CK2α' (IC50 = 1 nM). It shows greater than 500-fold selectivity for CK2 over a panel of > 200 kinases.

CX-4945 can be used, in combination with other small molecules, in fast chemical reprogramming protocols for the induction of human somatic cells and highly efficient generation of pluripotent stem cells (hCiPS) in a minimum of 16 days with robust repeatability and reliability.

CX-4945 has antiproliferative effects in vitro as it attenuates PI3K/Akt signalling, causes cell-cycle arrest and selectively induces apoptosis in cancer cells. In models of angiogenesis, CX-4945 inhibits human umbilical vein endothelial cell migration, tube formation, and blocks CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells.

In vivo, CX-4945 displays robust antitumor activity with concomitant reduction of the mechanism-based biomarker phospho-p21 (T145) (murine xenograft model). CX-4945 is orally bioavailable.

Product Specifications for CX-4945

Molecular Weight

371.76

Formula

C19H11ClN3O2Na

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

Sodium 5-[(3-Chlorophenyl)amino]benzo[c]-2,6-naphthyridine-8-carboxylate

CAS Number

1309357-15-0

InChI Key

ODDAAPQSODILSN-UHFFFAOYSA-M

SMILES

O=C(C1=CC(N=C(C2=C3C=NC=C2)NC4=CC(Cl)=CC=C4)=C3C=C1)O[Na]

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 37.18 100
DMSO 37.18 100

Preparing Stock Solutions for CX-4945

The following data is based on the product molecular weight 371.76.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.69 mL 13.45 mL 26.90 mL
5 mM 0.54 mL 2.69 mL 5.38 mL
10 mM 0.27 mL 1.34 mL 2.69 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Background References

References are publications that support the biological activity of the product.

Product Documents for CX-4945

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for CX-4945

For research use only

Related Research Areas

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