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ZW4864 free base

Catalog No. T9642 CAS 2632259-92-6

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 K i value of 0.76 μM and an IC 50 value of 0.87 μM [1]. ZW4864 (free base) shows good pharmacokinetic properties.

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ZW4864 free base, CAS 2632259-92-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 163.00
5 mg	In stock	$ 413.00
10 mg	In stock	$ 618.00
25 mg	In stock	$ 985.00
50 mg	In stock	$ 1,330.00
100 mg	In stock	$ 1,790.00
500 mg	In stock	$ 3,590.00
1 mL * 10 mM (in DMSO)	In stock	$ 455.00

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Purity: 99.54%

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Description	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 K i value of 0.76 μM and an IC 50 value of 0.87 μM [1]. ZW4864 (free base) shows 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].

Molecular Weight	570.72
Formula	C33H42N6O3
CAS No.	2632259-92-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (157.7 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library PPI Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Stem Cell Differentiation Compound Library Anti-Ovarian Cancer Compound Library Neuronal Differentiation Compound Library Anti-Cancer Metabolism Compound Library

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Keywords

ZW4864 free base 2632259-92-6 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin ZW-4864 ZW 4864 ZW4864 inhibitor inhibit

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