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CCT251545
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Catalog No. T14907Cas No. 1661839-45-7
CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).
CCT251545
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Purity: 98.69%
Catalog No. T14907Cas No. 1661839-45-7
CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $35 | In Stock | In Stock | |
| 5 mg | $81 | In Stock | In Stock | |
| 10 mg | $129 | In Stock | In Stock | |
| 25 mg | $263 | In Stock | In Stock | |
| 50 mg | $428 | In Stock | In Stock | |
| 100 mg | $689 | In Stock | In 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.
Batch Information
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Purity:98.69%
Appearance:Solid
Color:White to Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells). |
| Targets&IC50 | WNT (7dF3 cells):5 nM |
| In vitro | CCT251545, a small-molecule inhibitor of the WNT pathway discovered through cell-based screening, is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.?X-ray crystallography demonstrates a type 1 binding mode involving insertion of the CDK8 C terminus into the ligand binding site.?In contrast to type II inhibitors of CDK8 and CDK19, CCT251545 displays potent cell-based activity.?We show that CCT251545 and close analogs alter WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.?Consistent with this, we find that phosphorylation of STAT1(SER727) is a biomarker of CDK8 kinase activity in vitro and in vivo[1]. |
| In vivo | In vivo, CCT251545 with WNT-dependent tumors activity[1]. |
| Molecular Weight | 421.92 |
| Formula | C23H24ClN5O |
| Cas No. | 1661839-45-7 |
| Smiles | Cn1cc(cn1)-c1ccc(cc1)-c1cncc(Cl)c1N1CCC2(CCNC2=O)CC1 |
| Relative Density. | 1.37 g/cm3 (Predicted) |
| Storage | store 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: 1 mg/mL (2.37 mM), Sonication is recommended.  | ||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.37 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
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Calculator
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:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 μL PEG300 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 ddH2O 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.
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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