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CCT244747

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Catalog No. T14904Cas No. 1404095-34-6
Alias CCT 244747

CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.

CCT244747

CCT244747

😃Good
Purity: 99.17%
Catalog No. T14904Alias CCT 244747Cas No. 1404095-34-6
CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.
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1 mg$69-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.17%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.
Targets&IC50
Chk1:7.7 nM
In vitro
Methods: HT29 and SW620 colon cancer cell lines were treated with CCT244747 (0.01, 0.05, 0.1, 0.5, 1, 2, 5 μM) to characterize its effects on drug-induced changes in CHK1 and cell cycle biomarkers.
Results CCT244747 inhibited SN38- and gemcitabine-induced CHK1 activity in tumor cells, and this was associated with abrogation of cell cycle arrest, induction of DNA damage, and apoptosis. [4]
In vivo
Methods: Athymic mice bearing SW620 human colon cancer xenografts were treated with CCT244747 (100-300 mg/kg, oral) followed by gemcitabine (60 mg/kg, intravenous) 1 hour later to further analyze the pharmacodynamics of CCT244747.
Results: A single oral dose of CCT244747 (100-300 mg/kg) maintained inhibition of gemcitabine-induced pS296 CHK1 in HT29 colon tumor xenografts for up to 24 hours. [1]
SynonymsCCT 244747
Chemical Properties
Molecular Weight408.46
FormulaC20H24N8O2
Cas No.1404095-34-6
SmilesO(C)C=1C(=CN=C(NC2=NC(O[C@@H](CN(C)C)C)=C(C#N)N=C2)C1)C=3C=NN(C)C3
Relative Density.1.27 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 40 mg/mL (97.93 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.9 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 mM2.4482 mL12.2411 mL24.4822 mL122.4110 mL
5 mM0.4896 mL2.4482 mL4.8964 mL24.4822 mL
10 mM0.2448 mL1.2241 mL2.4482 mL12.2411 mL
20 mM0.1224 mL0.6121 mL1.2241 mL6.1206 mL
50 mM0.0490 mL0.2448 mL0.4896 mL2.4482 mL

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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:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
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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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