3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)-
![3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)- Structure](CAS/20210305/GIF/2632259-92-6.gif)
- CAS No.
- 2632259-92-6
- Chemical Name:
- 3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)-
- Synonyms
- ZW4864 free base;ZW4864 free base, 10 mM in DMSO;3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)-
- CBNumber:
- CB79741990
- Molecular Formula:
- C33H42N6O3
- Molecular Weight:
- 570.72
- MDL Number:
- MOL File:
- 2632259-92-6.mol
3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)- Properties
| Boiling point | 842.8±65.0 °C(Predicted) |
|---|---|
| Density | 1.28±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| form | Solid |
| pka | 13.86±0.50(Predicted) |
| color | Light yellow to yellow |
3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)- Chemical Properties,Uses,Production
Biological Activity
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[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]. ZW4864 (20 mg/kg; p.o.) (free base) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %[1].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].
References
[1]. Wang Z, et al. Discovery of an Orally Bioavailable Small-Molecule Inhibitor for the β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction. J Med Chem. 2021;64(16):12109-12131.
3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)- Preparation Products And Raw materials
Raw materials
Preparation Products
3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11974 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9266 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19699 | 58 |
| sangon@qq.com | CHINA | 47239 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 58 |
| RD International Technology Co., Limited | 58 |
| TargetMol Chemicals Inc. | 58 |
| 58 |
View Lastest Price from 3-Piperidinecarboxamide, N-cyclopropyl-1-[3-[1,1-dimethyl-2-oxo-2-(1-piperazinyl)ethoxy]phenyl]-N-[[4-(1H-pyrazol-4-yl)phenyl]methyl]-, (3R)- manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
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2024-11-19 | ZW4864 free base
2632259-92-6
|
US $163.00-618.00 / mg | 99.54% | 10g | TargetMol Chemicals Inc. |
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- ZW4864 free base
2632259-92-6
- US $163.00-618.00 / mg
- 99.54%
- TargetMol Chemicals Inc.