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CCT-251921
🥰Excellent
Catalog No. T14901Cas No. 1607837-31-9
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].
CCT-251921
🥰Excellent
Purity: 99.07%
Catalog No. T14901Cas No. 1607837-31-9
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $87 | In Stock | In Stock | |
| 5 mg | $233 | In Stock | In Stock | |
| 10 mg | $342 | In Stock | In Stock | |
| 25 mg | $577 | In Stock | In Stock | |
| 50 mg | $827 | In Stock | In Stock | |
| 100 mg | $1,130 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $213 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
Batch Information
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Purity:99.07%
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Product Introduction
Bioactivity
Chemical Properties
| Description | CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM]. |
| Targets&IC50 | CDK8:2.3 nM (IC50), CDK19:2.6 nM (IC50) |
| In vitro | CCT-251921 exhibits limited activity across a panel of 55 receptors, ion channels, and enzymes at 1 μM, as well as a panel of 279 kinases, while showing weak inhibition of CYPs. It effectively inhibits basal WNT pathway activity in human cancer cell lines with constitutive activation of WNT pathway signaling, specifically in LS174T (β-catenin mutant), SW480, and Colo205 (APC mutant) cell lines, and PA-1 human teratocarcinoma cells, which depend on WNT ligand. |
| In vivo | CCT-251921 exhibits enhanced oral pharmacokinetics and pharmaceutical properties, maintaining inhibition of STAT1SER727 phosphorylation for over 6 hours post-dose. In an APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduced tumor weight in mice by 54.2% on day 15. |
| Molecular Weight | 410.9 |
| Formula | C21H23ClN6O |
| Cas No. | 1607837-31-9 |
| Smiles | Cn1ncc2cc(ccc12)-c1cnc(N)c(Cl)c1N1CCC2(CCNC2=O)CC1 |
| Relative Density. | 1.51 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 15 mg/mL (36.51 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.87 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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