CCT251545

Catalog No.S7981 Batch:S798101

Technical Data

Formula	C₂₃H₂₄ClN₅O
Molecular Weight	421.92	CAS No.	1661839-45-7
Solubility (25°C)*	In vitro	DMSO	30 mg/mL (71.1 mM)
		Ethanol	5 mg/mL (11.85 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models Female NMRI mice, Male Wistar rats Dosages 0.2 mg/kg, 0.5 mg/kg Administration IV, Oral gavage

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
Female NMRI mice, Male Wistar rats
Dosages
0.2 mg/kg, 0.5 mg/kg
Administration
IV, Oral gavage

References

Selleck's CCT251545 has been cited by 3 publications

Enhanced T cell effector activity by targeting the Mediator kinase module [ Science, 2022, 378(6620):eabn5647]	PubMed: 36356142
RING-Finger Protein 6 promotes Drug Resistance in Retinoblastoma via JAK2/STAT3 Signaling Pathway [ Pathol Oncol Res, 2022, 28:1610273]	PubMed: 35369571
Antagonizing CDK8 Sensitizes Colorectal Cancer to Radiation Through Potentiating the Transcription of e2f1 Target Gene apaf1 [ Front Cell Dev Biol, 2020, 8:408]	PubMed: 32596239

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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