Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 87.00 | |
5 mg | In stock | $ 233.00 | |
10 mg | In stock | $ 342.00 | |
25 mg | In stock | $ 577.00 | |
50 mg | In stock | $ 827.00 | |
100 mg | In stock | $ 1,130.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 213.00 |
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 demonstrates minimal activity when tested in a panel of 55 receptors, ion channels, and enzymes at 1 μM and in a panel of 279 kinases. And weak inhibition of CYPs is observed. CCT-251921 demonstrates potent inhibition of reporter-based readouts measuring basal WNT pathway activity in human cancer cell lines that have constitutively activated WNT pathway signaling: LS174T (β-catenin mutant), SW480 and Colo205 (APC mutant) or PA-1 human teratocarcinoma cells that are WNT ligand-dependent. |
In vivo | CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties. The inhibition of STAT1SER727 phosphorylation is maintained for more than 6 h after the last dose. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) on day 15. |
Molecular Weight | 410.9 |
Formula | C21H23ClN6O |
CAS No. | 1607837-31-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.33 mg/mL (81.11 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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CCT-251921 1607837-31-9 Cell Cycle/Checkpoint CDK CCT251921 Cyclin dependent kinase Inhibitor inhibit CCT 251921 inhibitor