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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 |
Description | CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM]. |
Targets&IC50 | CDK19:2.6 nM (IC50), CDK8:2.3 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 |
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 | ||||||||||||||||||||||||||
DMSO
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