Silmitasertib (CX-4945) Sodium

Alias: CX-4945; CX 4945; CX4945 Sodium Salt
Cat No.:V2616 Purity: ≥98%
Silmitasertib(also know as CX-4945) is a selective and orally bioavailable small-molecule inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, it is less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay).
Silmitasertib (CX-4945) Sodium Chemical Structure CAS No.: 1309357-15-0
Product category: Casein Kinase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Silmitasertib (CX-4945) Sodium:

  • CX-4945 (Silmitasertib)
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Silmitasertib (also know as CX-4945) is a selective and orally bioavailable small-molecule inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, it is less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). CX-4945 selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2 is a protein kinase overexpressed in a variety of cancer cell types and is correlated with malignant transformation, tumor growth and survival.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Cell-cycle arrest and selective apoptosis in cancer cells as compared to normal cells are caused by silmitasertib (CX-4945), which also attenuates PI3K/Akt signaling. The antiproliferative activity of silmitasertib (CX-4945) is correlated with the expression levels of the CK2α catalytic subunit. In order to buffer the PS-341-mediated proteotoxic stress in the ER lumen, leukemic cells cannot engage a functional UPR. Silmitasertib (CX-4945) with PS-341 therapy reduces pro-survival ER chaperon BIP/Grp78 expression[2]. Activation of the CK2-mediated PI3K/Akt/mTOR signaling pathways is suppressed and cytotoxicity and apoptosis are induced in hematological malignancies by silmitasertib (CX-4945) via downregulating CK2 expression[3].
ln Vivo
In murine xenograft models, silmitasertib (CX-4945) (25 or 75 mg/kg, po) is well tolerated and has shown strong anticancer activity with simultaneous decreases in the mechanism-based biomarker phospho-p21 (T145)[1].
Animal Protocol
Dissolved in DMSO, and diluted in PBS; 25 or 75 mg/kg; Oral gavage
Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
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 Dec 15;70(24):10288-98.
[2]. Kendall JJ, et al. CK2 blockade causes MPNST cell apoptosis and promotes degradation of β-catenin. Oncotarget. 2016 Aug 16;7(33):53191-53203.
[3]. Buontempo F, et al. Synergistic cytotoxic effects of PS-341 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. Oncotarget. 2016 Jan 12;7(2):1323-40.
[4]. Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H11CLN3O2NA
Molecular Weight
371.75
CAS #
1309357-15-0
SMILES
O=C(C1=CC=C2C3=C(C(NC4=CC=CC(Cl)=C4)=NC2=C1)C=CN=C3)[O-].[Na+]
InChi Key
ODDAAPQSODILSN-UHFFFAOYSA-M
InChi Code
InChI=1S/C19H12ClN3O2.Na/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);/q;+1/p-1
Chemical Name
Sodium 5-[(3-Chlorophenyl)amino]-benzo[c]-2,6-naphthyridine-8-carboxylate
Synonyms
CX-4945; CX 4945; CX4945 Sodium Salt
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 10 mM
Water: N/A
Ethanol:N/A
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6900 mL 13.4499 mL 26.8998 mL
5 mM 0.5380 mL 2.6900 mL 5.3800 mL
10 mM 0.2690 mL 1.3450 mL 2.6900 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • CX-4945 Sodium

  • CX-4945 Sodium

Contact Us