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CCT251545 Wnt/beta-catenin inhibitor

Name: CCT251545
Brand: Selleck Chemicals
SKU: S7981
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S7981

CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. This compound also acts as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

Chemical Structure

Molecular Weight: 421.92

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Quality Control

Batch: Purity: 99.87%

99.87

Related Targets	JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase
Other Wnt/beta-catenin Products	ICG-001 IWR-1-endo IWP-2 Foscenvivint (PRI-724) Isoquercitrin Tegatrabetan (BC-2059) SKL2001 BML-284 (Wnt agonist 1) Salinomycin (from Streptomyces albus) FH535

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (71.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.200mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 84 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	421.92	Formula	C₂₃H₂₄ClN₅O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1661839-45-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1C=C(C=N1)C2=CC=C(C=C2)C3=CN=CC(=C3N4CCC5(CCNC5=O)CC4)Cl

Mechanism of Action

Targets/IC₅₀/Ki	CDK8 CDK19 Wnt (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. This compound 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 vivo	This compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25680029/ [2] https://pubmed.ncbi.nlm.nih.gov/26502155/

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