ZW4864
Based on 1 Customer Validation
ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.06%
- No. CAS: 2632259-93-7
- Fòrmula: C33H43ClN6O3
- Peso molecular:607.19
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
IC50: 0.87 μM (β catenin/BCL9 PPI)[1].
Ki: 0.76 μM(β catenin/BCL9 PPI)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
76 μM
Compound: 15; ZW4864
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Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
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[PMID: 34382808] |
| HCT-116 | IC50 |
76 μM
Compound: ZW4864
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured by MTS method
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[PMID: 35586435] |
| MCF-10A | IC50 |
92 μM
Compound: 15; ZW4864
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Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
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[PMID: 34382808] |
| MCF-10A | IC50 |
92 μM
Compound: ZW4864
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Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured by MTS method
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[PMID: 35586435] |
| MDA-MB-231 | IC50 |
28 μM
Compound: 15; ZW4864
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
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[PMID: 34382808] |
| MDA-MB-231 | IC50 |
28 μM
Compound: ZW4864
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured by MTS method
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[PMID: 35586435] |
| MDA-MB-468 | IC50 |
9.6 μM
Compound: 15; ZW4864
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Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
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[PMID: 34382808] |
| MDA-MB-468 | IC50 |
9.6 μM
Compound: ZW4864
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth measured by MTS method
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[PMID: 35586435] |
| SW480 | IC50 |
24 μM
Compound: 15; ZW4864
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Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
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[PMID: 34382808] |
| SW480 | IC50 |
24 μM
Compound: ZW4864
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Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth measured by MTS method
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[PMID: 35586435] |
In Vitro
ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) decreases the expression levels of Axin2 and cyclin D1 proteins[1].
ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A and MDA-MB-468 cells) selectively triggeres rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells[1].
ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) suppresses the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells[1].
ZW4864 binds with β-catenin and selectively disrupts the protein protein interaction (PPI) between B-cell lymphoma 9 (BCL9) and β-catenin while sparing the β-catenin/E-cadherin PPI. ZW4864 dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC50 of 11 μM. ZW4864 also dose-dependently suppresses the TOPFlash luciferase activities in SW480 and Wnt 3a-activated MDA-MB-468 cells with the IC50s of 7.0 and 6.3 μM, respectively. ZW4864 selectively suppresses transactivation of β-catenin signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480 and MBA-MD-231 cells
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Concentration:10~40 μM
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Incubation Time:24 hours
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Result:Decreased the expression levels of Axin2 and cyclin D1 proteins.
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Cell Line:MDA-MB231, MCF10A and MDA-MB-468 cells
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Concentration:10~40 μM
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Incubation Time:72 hours
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Result:Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.
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Cell Line:SW480 and MBA-MD-231 cells
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Concentration:10~40 μM
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Incubation Time:24 hours
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Result:Suppressed the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells.
In Vivo
ZW4864 (90 mg/kg; p.o.) shows a variation in tumor growth in mice[1].
ZW4864 shows good pharmacokinetic properties and effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2632259-93-7
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Appearance Solid
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Peso molecular 607.19
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Fòrmula C33H43ClN6O3
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Color White to off-white
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SMILES
O=C(N(CC1=CC=C(C=C1)C2=CNN=C2)C3CC3)[C@H]4CN(CCC4)C5=CC=CC(OC(C)(C(N6CC[NH2+]CC6)=O)C)=C5.[Cl-]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (82.35 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
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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 (sealed storage, away from moisture)
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
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 (sealed storage, away from moisture). 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 | 1.6469 mL | 8.2347 mL | 16.4693 mL | 41.1733 mL |
| 5 mM | 0.3294 mL | 1.6469 mL | 3.2939 mL | 8.2347 mL | |
| 10 mM | 0.1647 mL | 0.8235 mL | 1.6469 mL | 4.1173 mL | |
| 15 mM | 0.1098 mL | 0.5490 mL | 1.0980 mL | 2.7449 mL | |
| 20 mM | 0.0823 mL | 0.4117 mL | 0.8235 mL | 2.0587 mL | |
| 25 mM | 0.0659 mL | 0.3294 mL | 0.6588 mL | 1.6469 mL | |
| 30 mM | 0.0549 mL | 0.2745 mL | 0.5490 mL | 1.3724 mL | |
| 40 mM | 0.0412 mL | 0.2059 mL | 0.4117 mL | 1.0293 mL | |
| 50 mM | 0.0329 mL | 0.1647 mL | 0.3294 mL | 0.8235 mL | |
| 60 mM | 0.0274 mL | 0.1372 mL | 0.2745 mL | 0.6862 mL | |
| 80 mM | 0.0206 mL | 0.1029 mL | 0.2059 mL | 0.5147 mL |
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