ZW4864 free base
Based on 1 Customer Validation
ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.
For research use only. We do not sell to patients.
- Purity: 99.42%
- CAS No.: 2632259-92-6
- Formula: C33H42N6O3
- Molecular Weight:570.72
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 0.87 μM (β catenin/BCL9 PPI)[1].
Ki: 0.76 μM (β catenin/BCL9 PPI)[1]
ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) 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) (free base) 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) (free base) 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 (free base) 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 (free base) dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 (free base) suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC50 of 11 μM. ZW4864 (free base) 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 (free base) 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.
ZW4864 (90 mg/kg; p.o.) (free base) shows a variation in tumor growth in mice[1].
ZW4864 (free base) 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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CAS No. 2632259-92-6
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Appearance Solid
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Molecular Weight 570.72
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Formula C33H42N6O3
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Color Light yellow to yellow
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SMILES
O=C([C@H]1CN(C2=CC=CC(OC(C)(C)C(N3CCNCC3)=O)=C2)CCC1)N(C4CC4)CC5=CC=C(C6=CNN=C6)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (175.22 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. 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. 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)
Purity & Documentation
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Data Sheet (275 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 1.7522 mL | 8.7609 mL | 17.5217 mL | 43.8043 mL |
| 5 mM | 0.3504 mL | 1.7522 mL | 3.5043 mL | 8.7609 mL | |
| 10 mM | 0.1752 mL | 0.8761 mL | 1.7522 mL | 4.3804 mL | |
| 15 mM | 0.1168 mL | 0.5841 mL | 1.1681 mL | 2.9203 mL | |
| 20 mM | 0.0876 mL | 0.4380 mL | 0.8761 mL | 2.1902 mL | |
| 25 mM | 0.0701 mL | 0.3504 mL | 0.7009 mL | 1.7522 mL | |
| 30 mM | 0.0584 mL | 0.2920 mL | 0.5841 mL | 1.4601 mL | |
| 40 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0951 mL | |
| 50 mM | 0.0350 mL | 0.1752 mL | 0.3504 mL | 0.8761 mL | |
| 60 mM | 0.0292 mL | 0.1460 mL | 0.2920 mL | 0.7301 mL | |
| 80 mM | 0.0219 mL | 0.1095 mL | 0.2190 mL | 0.5476 mL | |
| 100 mM | 0.0175 mL | 0.0876 mL | 0.1752 mL | 0.4380 mL |
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