E722-2648 TFA

Cat. No.: HY-148918A Purity: 96.33%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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E722-2648 TFA is an inhibitor targeting the BCL9 and β-catenin complex with antitumor activity. E722-2648 TFA blocks complex formation by disrupting the interaction between the two proteins, thereby inhibiting β-catenin-mediated transcriptional activity and downregulating the expression of WNT target genes. E722-2648 TFA effectively inhibits tumor growth in colon cancer xenograft models and colorectal cancer mouse models. E722-2648 TFA can be used for the research of colon cancer and colorectal cancer.

For research use only. We do not sell to patients.

E722-2648 TFA Chemical Structure

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MOQ		Minimum order quantity
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This product is a controlled substance and not for sale in your territory.

Other Forms of E722-2648 TFA:

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•Related Small Molecules:

•Related Proteins:

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Wnt1 Wnt3 Wnt5 Wnt7 Wnt11

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

E722-2648 TFA (1-20 μM; 16 h) dose-dependently inhibits the formation of endogenous β-catenin/BCL9 complexes in Colo320 and HCT116 colorectal cancer cells, without disrupting the interaction between β-catenin and E-cadherin, and exhibits excellent target specificity^[1].
E722-2648 TFA (6.25-25 μM; 16 h) dose-dependently inhibits the transcriptional activity of the Wnt/β-catenin pathway in dual-luciferase reporter assays using Colo320 and HCT116 colorectal cancer cells^[1].
E722-2648 TFA (10 μM, 20 μM; 6-48 h) downregulates the mRNA expression levels of Wnt pathway target genes AXIN2 and CD44 in a time- and dose-dependent manner in Colo320 and HCT116 colorectal cancer cells^[1].
E722-2648 TFA (25-50 μM; 24 h) dose-dependently downregulates the mRNA expression levels of Wnt pathway target genes AXIN2, CD44, and LGR5 in human neoplastic colon organoids carrying the APC gene c.4778delA mutation^[1].
E722-2648 TFA (5-20 μM; 24-48 h) dose-dependently downregulates the protein expression levels of AXIN2, CD44 and active β-catenin, and simultaneously increases the level of cleaved PARP to induce apoptosis in Colo320 and HCT116 colorectal cancer cells, whereas it exerts no such effects on β-catenin-independent RKO cells^[1].
E722-2648 TFA (20 μM; 48 h) significantly reduces the viability of HCT116 and Colo320 colorectal cancer cells. The decrease in cell viability becomes more pronounced when combined with the Wnt inhibitor ICG-001, the cholesterol synthesis inhibitor Lovastatin (HY-N0504), and the cholesterol esterification inhibitor Avasimibe (HY-13215). Exogenous cholesterol supplementation partially rescues the reduction in cell viability induced by E722-2648 TFA treatment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

E722-2648 (4 mg/kg; i.p.; administered once every other day for 20 days) TFA significantly reduces the weight and volume of intraperitoneal tumors in mice, exerting potent in vivo anti-colorectal cancer activity in a mouse intraperitoneal xenograft model of colorectal cancer established with HCT116 cells^[1].
E722-2648 (3 mg/kg; intratumoral injection; administered once every other day for 20 days) TFA significantly inhibits subcutaneous tumor growth, reduces tumor weight and GFP fluorescence signals in tumor tissues, downregulates the expression of Wnt pathway target genes AXIN2 and CD44 in tumor tissues, suppresses tumor cell proliferation and tumor angiogenesis, induces tumor cell apoptosis, and decreases the infiltration of pro-tumor M2-like tumor-associated macrophages in the subcutaneous colorectal cancer xenograft model of NCr nude mice bearing HCT116-GFP cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

504.63

Formula

C₂₃H₃₁F₃N₂O₃S₂

Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(C1=CC(SC2=C3CCCC2)=C3CS1)NCCCN4CCCC(C4)C.OC(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (198.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9816 mL	9.9082 mL	19.8165 mL
5 mM	0.3963 mL	1.9816 mL	3.9633 mL
10 mM	0.1982 mL	0.9908 mL	1.9816 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 96.33%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (248 KB) HNMR (221 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Groenewald W, et al. The Role of WNT Pathway Mutations in Cancer Development and an Overview of Therapeutic Options. Cells. 2023;12(7):990. Published 2023 Mar 24. [Content Brief]

[2]. Cao M, et al. Classical Angiogenic Signaling Pathways and Novel Anti-Angiogenic Strategies for Colorectal Cancer. Curr Issues Mol Biol. 2022;44(10):4447-4471. Published 2022 Sep 26. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9816 mL	9.9082 mL	19.8165 mL	49.5412 mL
	5 mM	0.3963 mL	1.9816 mL	3.9633 mL	9.9082 mL
	10 mM	0.1982 mL	0.9908 mL	1.9816 mL	4.9541 mL
	15 mM	0.1321 mL	0.6605 mL	1.3211 mL	3.3027 mL
	20 mM	0.0991 mL	0.4954 mL	0.9908 mL	2.4771 mL
	25 mM	0.0793 mL	0.3963 mL	0.7927 mL	1.9816 mL
	30 mM	0.0661 mL	0.3303 mL	0.6605 mL	1.6514 mL
	40 mM	0.0495 mL	0.2477 mL	0.4954 mL	1.2385 mL
	50 mM	0.0396 mL	0.1982 mL	0.3963 mL	0.9908 mL
	60 mM	0.0330 mL	0.1651 mL	0.3303 mL	0.8257 mL
	80 mM	0.0248 mL	0.1239 mL	0.2477 mL	0.6193 mL
	100 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.4954 mL

E722-2648 TFA Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E722-2648β-cateninWntBcl-2 FamilyBeta cateninInhibitorinhibitorinhibit

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