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CK2 inhibitor 2

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Catalog No. T35557Cas No. 2641079-92-5

CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM. It exhibits high selectivity towards Clk2 with an IC50 of 32.69 nM in comparison to CK2. Furthermore, CK2 Inhibitor 2 has been shown to possess promising antiproliferative and antitumor activities [1].

CK2 inhibitor 2

CK2 inhibitor 2

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🥰Excellent
Purity: 99.02%
Catalog No. T35557Cas No. 2641079-92-5
CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM. It exhibits high selectivity towards Clk2 with an IC50 of 32.69 nM in comparison to CK2. Furthermore, CK2 Inhibitor 2 has been shown to possess promising antiproliferative and antitumor activities [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$59In StockIn Stock
5 mg$148In StockIn Stock
10 mg$238In StockIn Stock
25 mg$473In StockIn Stock
50 mg$708In StockIn Stock
100 mg$948In StockIn Stock
200 mg$1,280In StockIn Stock
1 mL x 10 mM (in DMSO)$163In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.02%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM. It exhibits high selectivity towards Clk2 with an IC50 of 32.69 nM in comparison to CK2. Furthermore, CK2 Inhibitor 2 has been shown to possess promising antiproliferative and antitumor activities [1].
Targets&IC50
CK2:0.66 nM, CLK2/CK2:32.69 nM
In vitro
CK2 inhibitor 2 (compound 1c) effectively inhibits the proliferation of PC-3, HCT-116, MCF-7, HT-29, T24, and LO2 cancer cell lines with IC50 values of 4.53 μM, 3.07 μM, 7.50 μM, 5.18 μM, 6.10 μM, and 96.68 μM, respectively. It induces dose-dependent apoptosis in HCT-116 cells, achieving a 55% apoptotic ratio at 20 μM after 24 hours. The compound reduces phosphorylated Akt1 S129 and Cdc37 S13 expression, suggesting suppression of survival pathways. It also inhibits ALDH1A1 enzyme activity (IC50 of 0.10 μM) and downregulates its transcription and protein expression in HCT-116 cells, indicating potential for targeting cancer-specific metabolic pathways.
In vivo
Administering CK2 inhibitor 2 at doses ranging from 60 to 90 mg/kg orally, twice daily for four weeks, significantly inhibits tumor growth in a dose-dependent manner, achieving a peak inhibition rate of 69% at the 90 mg/kg dosage. A single oral dose of 25 mg/kg in Sprague-Dawley rats reveals pharmacokinetic parameters such as a maximum concentration (C max) of 7017.8 ng/mL, an elimination half-life (t 1/2) of 6.67 hours, and a clearance rate (CL) of 0.60 L/h/kg. The study utilized male BALB/c athymic nude mice, aged 5 weeks and weighing 16-18 grams, injected with HCT-116 cells, demonstrating dose-dependent tumor growth inhibition without noticeable changes in body weight.
Chemical Properties
Molecular Weight392.84
FormulaC21H17ClN4O2
Cas No.2641079-92-5
SmilesN(C1=C2C(=C3C(=N1)C=C(C(NCCO)=O)C=C3)C=NC=C2)C4=CC(Cl)=CC=C4
Relative Density.1.420 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (127.28 mM), Sonication and heating to 60℃ are recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 2.5 mg/mL (6.36 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5456 mL12.7278 mL25.4557 mL127.2783 mL
5 mM0.5091 mL2.5456 mL5.0911 mL25.4557 mL
10 mM0.2546 mL1.2728 mL2.5456 mL12.7278 mL
20 mM0.1273 mL0.6364 mL1.2728 mL6.3639 mL
50 mM0.0509 mL0.2546 mL0.5091 mL2.5456 mL
100 mM0.0255 mL0.1273 mL0.2546 mL1.2728 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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