Home Tools

ZW4864

Catalog No. T40256 CAS 2632259-93-7

ZW4864 is a selective inhibitor of the β-catenin/B-Cell Lymphoma 9 protein (β-catenin/BCL9 PPI) interaction, demonstrating oral activity. It inhibits β-catenin/BCL9 PPI with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

ZW4864, CAS 2632259-93-7

Please contact us for prices and availability for the specification of product you are interested at.
Product consultation

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ZW4864 is a selective inhibitor of the β-catenin/B-Cell Lymphoma 9 protein (β-catenin/BCL9 PPI) interaction, demonstrating oral activity. It inhibits β-catenin/BCL9 PPI with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM.
Targets&IC50	β-catenin-BCL9:0.76 μM (Ki), β-catenin-BCL9:0.87 μM (IC50)
In vitro	ZW4864, at concentrations ranging from 10 to 40 μM over periods of 24 to 72 hours, has been demonstrated to modulate β-catenin signaling pathways selectively in various cell lines, including SW480, MDA-MB-231, MDA-MB-468, and MCF10A. Specifically, it lowers the levels of Axin2 and cyclin D1 proteins in SW480 and MDA-MD-231 cells, demonstrating a suppression of β-catenin target gene transcription without impacting the expression of the housekeeper gene HPRT. Furthermore, ZW4864 is effective in inducing rapid apoptosis in triple-negative breast cancer cells that exhibit hyperactive β-catenin signaling, leaving normal MCF10A mammary epithelial cells unaffected. Its mechanism of action includes binding to β-catenin, disrupting its interaction with B-cell lymphoma 9 (BCL9) but not with E-cadherin, thus inhibiting β-catenin signaling pathway activation, downregulating oncogenic target genes, and reducing cancer cell invasiveness. This compound also significantly diminishes TOPFlash luciferase activity in a dose-dependent manner in β-catenin-expressing cells, indicating a targeted suppression of β-catenin transactivation. These findings, validated through Western Blot Analysis, Apoptosis Analysis, and RT-PCR, underscore ZW4864's potential as a selective inhibitor of β-catenin signaling in cancer research.
In vivo	ZW4864, administered orally at a dosage of 20 mg/kg, demonstrates favorable pharmacokinetic properties, achieving an oral bioavailability (F) of 83%[1]. At a higher dosage of 90 mg/kg, the compound is observed to alter tumor growth in mice[1]. Furthermore, ZW4864 effectively inhibits β-catenin target gene expression within a patient-derived xenograft mouse model. These studies were conducted using C57BL/6 mice for pharmacokinetic analysis at 20 mg/kg dosage and general mice population at 90 mg/kg dosage, showcasing the compound's potential in moderating tumor progression and exhibiting excellent pharmacokinetic profiles[1].

Molecular Weight	607.2
Formula	C33H43ClN6O3
CAS No.	2632259-93-7

Storage

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

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.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ZW4864 2632259-93-7 ZW 4864 ZW-4864 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.