[CAS NO. 1607837-31-9] CCT-251921
PRODUCTS SPECIFICATIONS [1607837-31-9]
DESCRIPTION [1607837-31-9]
Overview
| MDL | MFCD30502895 |
|---|---|
| Molecular Weight | 410.90 |
| Molecular Formula | C21H23ClN6O |
| SMILES | O=C1NCCC12CCN(C3=C(Cl)C(N)=NC=C3C4=CC5=C(N(C)N=C5)C=C4)CC2 |
1 Publications Citing Use of MCE
Summary
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC 50 of 2.3 nM.
IC50 & Target
|
CDK8 2.3 nM (IC 50 ) |
CDK19 2.6 nM (IC 50 ) |
In Vitro
CCT-251921 has acceptable aqueous solubility and 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; 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties in order to facilitate further evaluation of CDK8/19 pharmacology and progression into preclinical efficacy and safety studies. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) at day 15. The inhibition of STAT1 SER727 phosphorylation is maintained for more than 6 h after the last dose [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 81.11 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4337 mL | 12.1684 mL | 24.3368 mL |
| 5 mM | 0.4867 mL | 2.4337 mL | 4.8674 mL |
| 10 mM | 0.2434 mL | 1.2168 mL | 2.4337 mL |