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iCRT14 Wnt/beta-catenin inhibitor

Name: iCRT14
Brand: Selleck Chemicals
SKU: S8704
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S8704

iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.

Chemical Structure

Molecular Weight: 375.44

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S870401 DMSO]37 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.86%

99.86

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Chemical Information, Storage & Stability

Molecular Weight	375.44	Formula	C₂₁H₁₇N₃O₂S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	677331-12-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC(=C(N1C2=CN=CC=C2)C)C=C3C(=O)N(C(=O)S3)C4=CC=CC=C4

Solubility

In vitro
Batch:

DMSO : 37 mg/mL ( (98.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.	2.000mg/ml (5.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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.	2.000mg/ml (5.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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.

Mechanism of Action

Targets/IC₅₀/Ki	β-catenin/Tcf ^[1] 54 μM(Ki)
In vitro	iCRT14 suppresses the transcriptional activity of canonical Wnt signaling, downregulates Wnt/β-catenin-induced target genes, and inhibits the growth of colorectal cancer cells in vitro^[1]. This compound shows a modest reduction in the amount of Dvl but has no effect on Dvl phosphorylation itself. It inhibits the Wnt responsive STF16-luc reporter in mammalian HEK293 cells with an IC50 of 40.3 nM. This chemical can also interfere with TCF binding to DNA in addition to its ability to influence TCF-β-catenin interaction^[2].
In vivo	Administration of iCRT14 to the HCT116 and HT29 xenograft models reveals a marked decrease in CycD1, coincided with reduced proliferation of the tumors. Furthermore, these effects are correlated with a marked reduction (∼50%) in the initial growth rate of tumors within the first 3 wk (∼day 19) of this compound administration. After day 19, however, the rate of tumor growth is comparable with that of DMSO-treated control. Throughout the course of the study, the mice does not display any signs of systemic toxicity or weight loss that would indicate off-target or nonspecific effects. This compound may be metabolized rapidly in vivo, thus reducing its bioavailability^[2].
References	https://pubmed.ncbi.nlm.nih.gov/25985283/ https://pubmed.ncbi.nlm.nih.gov/21393571/

Applications

Methods	Biomarkers	Images	PMID
Western blot	BIRC5 / Myc / Axin2 caspase 3 / cleaved caspase 3 / cleaved PARP Snail / pS9-GSK-3β / GSK-3β / Akt1 / Akt2		24995804
Growth inhibition assay	Cell viability		24995804