Art. -Nr.: HY-132300

ZW4864

Name: ZW4864
Brand: MedChemExpress
SKU: HY-132300
Price: 500.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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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 K_i value of 0.76 μM and an IC₅₀ value of 0.87 μM.

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Reinheit: 98.06%
CAS. Nr.: 2632259-93-7
Formel: C₃₃H₄₃ClN₆O₃
Molecular Weight:607.19

Speicherung:

4°C, sealed storage, away from moisture

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

ZW4864 Chemical Structure

CAS. Nr.: 2632259-93-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	76 μM Compound: 15; ZW4864	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
HCT-116	IC₅₀	76 μM Compound: ZW4864	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured by MTS method Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured by MTS method	[PMID: 35586435]
MCF-10A	IC₅₀	92 μM Compound: 15; ZW4864	Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
MCF-10A	IC₅₀	92 μM Compound: ZW4864	Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured by MTS method Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured by MTS method	[PMID: 35586435]
MDA-MB-231	IC₅₀	28 μM Compound: 15; ZW4864	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
MDA-MB-231	IC₅₀	28 μM Compound: ZW4864	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured by MTS method Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured by MTS method	[PMID: 35586435]
MDA-MB-468	IC₅₀	9.6 μM Compound: 15; ZW4864	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
MDA-MB-468	IC₅₀	9.6 μM Compound: ZW4864	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth measured by MTS method Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth measured by MTS method	[PMID: 35586435]
SW480	IC₅₀	24 μM Compound: 15; ZW4864	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
SW480	IC₅₀	24 μM Compound: ZW4864	Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth measured by MTS method Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth measured by MTS method	[PMID: 35586435]

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.

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.

Chemical Information

CAS. Nr. 2632259-93-7
Appearance Solid
Molecular Weight 607.19
Formel C₃₃H₄₃ClN₆O₃
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-]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (82.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6469 mL

8.2347 mL

16.4693 mL

5 mM

0.3294 mL

1.6469 mL

3.2939 mL

10 mM

0.1647 mL

0.8235 mL

1.6469 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
	80 mM	0.0206 mL	0.1029 mL	0.2059 mL	0.5147 mL

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ZW4864

Tegatrabetan

ICG-001

NRX-252262

CWP232228

C004019

WAY-262611

β-catenin-IN-2

NRX-103094

ZW4864 free base

NRX-103095

NRX-2663

Tegatrabetan (Standard)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

ZW4864

Tegatrabetan

ICG-001

NRX-252262

CWP232228

C004019

WAY-262611

β-catenin-IN-2

NRX-103094

ZW4864 free base

NRX-103095

NRX-2663

Tegatrabetan (Standard)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ZW4864 Related Classifications

HY-132300 Related Classifications

Bioz