CCT251545 (C09-0823-225)

InformationCCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.TargetsCDK8 ; CDK19 ; Wnt (in 7dF3 cells) ; 5 nMIn vitroThe suppression of the WNT pathway activity by CCT251545 is not unique to a specific cell line, is independent of exogenous WNT pathway stimulation, does not result from destabilization of TCF1 or TCF4, and is not due to interference with the luciferase-based reporter readout. CCT251545 also demonstrates a lack of transporter-mediated efflux and a lack of activity across broad in vitro panels of enzyme, receptor, and ion channel targets.In vivoCCT251545 is a potent small-molecule inhibitor of WNT signaling with good oral pharmacokinetics. We demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing.Cell Research(from reference)Cell lines：7dF3 cells, HEK293 cells, SW480, LS174T, COLO205 human colorectal cancer cells Concentrations：9.1 μM - 0.068 nM Incubation Time：2 h, 6 h. Specification: 0.99 Molecular Formula: C23H24ClN5O Molecular Weight: 421.92 PubChem CID: 77050682 Isomeric SMILES: CN1C=C(C=N1)C2=CC=C(C=C2)C3=CN=CC(=C3N4CCC5(CCNC5=O)CC4)Cl