Home Stem Cells & Wnt Wnt/beta-catenin inhibitor - CDK modulator CCT251545 For research use only.

CCT251545

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.

CCT251545 Chemical Structure

CCT251545 Chemical Structure

CAS No. 1661839-45-7

Purity & Quality Control

CCT251545 Related Products

Signaling Pathway

Wnt/beta-catenin Signaling Pathways

Wnt/beta-catenin Signaling Pathway

Biological Activity

Description 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.
Targets
CDK8 [2] CDK19 [2] Wnt [1]
(in 7dF3 cells)
5 nM
In vitro
In vitro

The 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.[1]
Cell Research 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
Method

Taqman Assays. 7dF3 cells are seeded at 20 000 cells/well into 96-well cell culture plates. After overnight incubation the cells are treated with CCT251545 at concentrations ranging from 9.1 μM to 0.068 nM. After 2 or 6 h of incubation, cells are washed with PBS and stored at −80 ℃. Cells are lysed in Cells-to-cDNA II Cell lysis buffer and transferred to PCR plates.
In Vivo
In vivo

CCT251545 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.[1]
Animal Research Animal Models Female NMRI mice, Male Wistar rats
Dosages 0.2 mg/kg, 0.5 mg/kg
Administration IV, Oral gavage

Chemical Information & Solubility

Molecular Weight 421.92 Formula

C23H24ClN5O
CAS No. 1661839-45-7 SDF --
Smiles CN1C=C(C=N1)C2=CC=C(C=C2)C3=CN=CC(=C3N4CCC5(CCNC5=O)CC4)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 30 mg/mL ( (71.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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