ZW4864 free base NEW
| Price | $163 | $413 | $618 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: ZW4864 free base | CAS No.: 2632259-92-6 |
| Purity: 99.54% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | ZW4864 free base |
| Description | ZW4864 (free base) is an orally active and selective β-catenin/B-Cell lymphoma 9 protein-protein interaction (β-catenin/BCL9 PPI) inhibitor, with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM [1]. ZW4864 (free base) also demonstrates good pharmacokinetic properties. |
| In vitro | ZW4864 (10~40 μM; free base) demonstrates a multifaceted inhibitory effect on β-catenin signaling pathways in various cancer cell lines. Over 24 hours, it diminishes Axin2 and cyclin D1 protein levels in SW480 and MDA-MB-231 cells, and selectively induces apoptosis in triple-negative breast cancer cells (MDA-MB231, MDA-MB-468) with hyperactive β-catenin, sparing normal MCF10A cells, over 72 hours. It also decreases the transcription of β-catenin target genes without affecting HPRT expression, indicating specificity in its action. By binding to β-catenin, ZW4864 disrupts its interaction with BCL9 but not with E-cadherin, thereby selectively targeting β-catenin's oncogenic activity. This compound efficaciously suppresses β-catenin-dependent signaling and invasiveness of cancer cells, as well as TOPFlash luciferase activity in a dose-dependent manner, showing particular potency with IC50 values ranging from 6.3 to 11 μM across different cell lines. Collectively, these findings underscore ZW4864's potential as a targeted therapeutic agent against β-catenin-dependent malignancies. |
| In vivo | Administered orally at a dosage of 20 mg/kg, ZW4864 (free base) displays favorable pharmacokinetic properties, achieving an oral bioavailability of 83% in C57BL/6 mice [1]. At a higher dosage of 90 mg/kg, also administered orally, it demonstrates the ability to influence tumor growth in mice [1]. Additionally, ZW4864 (free base) effectively inhibits β-catenin target gene expression in a patient-derived xenograft mouse model, further indicating its potential therapeutic benefits [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 90.0 mg/mL (157.7 mM), Sonication is recommended. |
| Keywords | ZW4864 free base | ZW-4864 | ZW 4864 | ZW4864 |
| Inhibitors Related | Urea | PRI-724 | Wnt pathway activator 1 | L-quebrachitol | MSAB | EMT inhibitor-1 | Wogonin | CHIR-99021 | XAV-939 | Nefopam hydrochloride | KY-05009 | Bisdemethoxycurcumin |
| Related Compound Libraries | Bioactive Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | Neuroprotective Compound Library | Stem Cell Differentiation Compound Library | PPI Inhibitor Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Neuronal Differentiation Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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