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iCRT14

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

Catalog No.S8704 Purity:99.86%

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

iCRT14 Chemical Structure

CAS No. 677331-12-3

Purity & Quality Control

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

99.86

iCRT14 Related Products

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Signaling Pathway

Wnt/beta-catenin Signaling Pathway

Biological Activity

Description

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

Targets

β-catenin/Tcf ^[1]

54 μM(Ki)

In vitro
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]. iCRT14 shows a modest reduction in the amount of Dvl but has no effect on Dvl phosphorylation itself. iCRT14 inhibits the Wnt responsive STF16-luc reporter in mammalian HEK293 cells with an IC50 of 40.3 nM. iCRT14 can also interfere with TCF binding to DNA in addition to its ability to influence TCF-β-catenin interaction^[2].
Cell Research	Cell lines	Rat2 cells
	Concentrations	25 and 50 μM
	Incubation Time	2 h
	Method	Rat2 cells are pretreated with iCRTs at the indicated doses and stimulated for 2 h with Wnt3a or Wnt5a. Cell lysate is harvested for western analysis of Dvl2 phosphorylation.
Experimental Result Images	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

In Vivo
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 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. The compound may be metabolized rapidly in vivo, thus reducing its bioavailability^[2].
Animal Research	Animal Models	HCT116 and HT29 xenograft models (implanted tumor cells in athymic nude mice)
	Dosages	50 mg/kg
	Administration	i.p.

References

Chemical Information & Solubility

Molecular Weight	375.44	Formula	C₂₁H₁₇N₃O₂S
CAS No.	677331-12-3	SDF	--
Smiles	CC1=CC(=C(N1C2=CN=CC=C2)C)C=C3C(=O)N(C(=O)S3)C4=CC=CC=C4
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.0mg/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.	In vivo Formulation Calculator
Clear solution	5% DMSO 1 95% Corn oil	2.0mg/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.
Homogeneous suspension	CMC-NA	5.0mg/ml (13.32mM)	Homogeneous suspension for Oral and Intraperitoneal Injection. 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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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