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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: 97.74%
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $87 | In Stock | |
| 5 mg | $233 | In Stock | |
| 10 mg | $342 | In Stock | |
| 25 mg | $577 | In Stock | |
| 50 mg | $827 | In Stock | |
| 100 mg | $1,130 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $213 | In Stock |
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Purity:97.74%
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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.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. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 15 mg/mL (36.51 mM), Sonication is recommended.  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
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DMSO+30% PEG300+5% Tween 80+60% 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 μLddH2O 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 μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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