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CCT251545
🥰Excellent
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
🥰Excellent
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]
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Batch Information
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Purity:98.69%
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Product Introduction
Bioactivity
Chemical Properties
| 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) |
| Color | White |
| Appearance | Solid |
Storage & Solubility Information
| 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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals 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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