2. Stem Cell/Wnt
  3. β-catenin
  4. ZW4864

ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.

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ZW4864 Chemical Structure

ZW4864 Chemical Structure

CAS No. : 2632259-93-7

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Based on 1 publication(s) in Google Scholar

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ZW4864 Related Antibodies

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Description

ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM[1].

IC50 & Target

IC50: 0.87 μM (β catenin/BCL9 PPI)[1].
Ki: 0.76 μM(β catenin/BCL9 PPI)[1]
In Vitro

ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) 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) 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) 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 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 dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC50 of 11 μM. ZW4864 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 selectively suppresses transactivation of β-catenin signaling[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZW4864 Related Antibodies

Western Blot Analysis[1]

Cell Line: SW480 and MBA-MD-231 cells
Concentration: 10~40 μM
Incubation Time: 24 hours
Result: Decreased the expression levels of Axin2 and cyclin D1 proteins.

Apoptosis Analysis[1]

Cell Line: MDA-MB231, MCF10A and MDA-MB-468 cells
Concentration: 10~40 μM
Incubation Time: 72 hours
Result: Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.

RT-PCR[1]

Cell Line: SW480 and MBA-MD-231 cells
Concentration: 10~40 μM
Incubation Time: 24 hours
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.
In Vivo

ZW4864 (20 mg/kg; p.o.) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %[1].
ZW4864 (90 mg/kg; p.o.) shows a variation in tumor growth in mice[1].
ZW4864 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.

Animal Model: C57BL/6 mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.
Animal Model: Mice[1]
Dosage: 90 mg/kg
Administration: P.o.
Result: Showed a variation in tumor growth in mice.
Molecular Weight

607.19

Formula

C33H43ClN6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(CC1=CC=C(C=C1)C2=CNN=C2)C3CC3)[C@H]4CN(CCC4)C5=CC=CC(OC(C)(C(N6CC[NH2+]CC6)=O)C)=C5.[Cl-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (68.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6469 mL 8.2347 mL 16.4693 mL
5 mM 0.3294 mL 1.6469 mL 3.2939 mL
View the 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 (sealed storage, away from moisture). 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 1.6469 mL 8.2347 mL 16.4693 mL 41.1733 mL
5 mM 0.3294 mL 1.6469 mL 3.2939 mL 8.2347 mL
10 mM 0.1647 mL 0.8235 mL 1.6469 mL 4.1173 mL
15 mM 0.1098 mL 0.5490 mL 1.0980 mL 2.7449 mL
20 mM 0.0823 mL 0.4117 mL 0.8235 mL 2.0587 mL
25 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6469 mL
30 mM 0.0549 mL 0.2745 mL 0.5490 mL 1.3724 mL
40 mM 0.0412 mL 0.2059 mL 0.4117 mL 1.0293 mL
50 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8235 mL
60 mM 0.0274 mL 0.1372 mL 0.2745 mL 0.6862 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZW48642632259-93-7ZW 4864ZW-4864β-cateninBeta cateninorallyactiveselectiveβ cateninB-CelllymphomaproteininteractionInhibitorinhibitorinhibit

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