CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO:33.33 mg/mL (81.11 mM)

CDK8:2.3 nM (IC50), CDK19:2.6 nM (IC50)

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.

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.