E722-2648 TFA
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.
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- Purity: 96.33%
- 화학식: C23H31F3N2O3S2
- 분자량:504.63
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보관:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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.
Chemical Information
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Appearance Solid
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분자량 504.63
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화학식 C23H31F3N2O3S2
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Color Light yellow to brown
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SMILES
O=C(C1=CC(SC2=C3CCCC2)=C3CS1)NCCCN4CCCC(C4)C.OC(C(F)(F)F)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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
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.
| 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
HY-148918A Related Classifications
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