WZ811
Based on 3 publication(s) in Google Scholar
WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.80%
- No. CAS: 55778-02-4
- Fòrmula: C18H18N4
- Peso molecular:290.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) WZ811
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Actividad biológica
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CXCR4 0.3 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | EC50 |
0.3 nM
Compound: 32, WZ811
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Displacement of biotinylated TN14003 from CXCR4 in MDA-MB-231 cells
Displacement of biotinylated TN14003 from CXCR4 in MDA-MB-231 cells
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[PMID: 17958344] |
| MDA-MB-231 | EC50 |
5.2 nM
Compound: 32, WZ811
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Inhibition of SDF1-mediated invasion of human MDA-MB-231 cells
Inhibition of SDF1-mediated invasion of human MDA-MB-231 cells
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[PMID: 17958344] |
| U-87MG ATCC | IC50 |
1.8 nM
Compound: 5, WZ811
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Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis
Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis
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[PMID: 21105715] |
WZ811 (Compound 32) is a potent CXCR4 antagonist, effectively inhibits TN14003 binding to CXCR4, with an EC50 of 0.3 nM[1].
WZ811 blocks SDF-1 mediated modulation cAMP levels in U87 glioma cells (EC50=1.2 nM) and Matirgel infiltration of MDA-MB-231 cells (EC50=5.2 nM)[1].
WZ811 (1-40 μM) inhibits TF-1 and UT-7 cells proliferation in a dose dependent manner both after treatment for 24 h and 48 h. Moreover, WZ811 (5 μM) induces cell apoptosis and enhances the sensitivity of cells to docetaxel. In addition, WZ811 inhibits aggressiveness markers and induces apoptosis in chronic lymphocytic leukemia cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 55778-02-4
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Appearance Solid
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Peso molecular 290.36
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Fòrmula C18H18N4
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Color White to off-white
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SMILES
C1(CNC2=NC=CC=C2)=CC=C(CNC3=NC=CC=C3)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Rep
Ischemic stroke outcome after promoting CD4+CD25+ Treg cell migration through CCR4 overexpression in a tMCAO animal model. [Abstract]2024 May 3;14(1):10201. PMID: 38702399 -
Br J Haematol
CXCR4 antagonists disrupt leukaemia-meningeal cell adhesion and attenuate chemoresistance. [Abstract]2023 May;201(3):459-469. PMID: 36535585 -
Dis Markers
Identification of CXCR4 Upregulation in Diffuse Large B-Cell Lymphoma Associated with Prognostic Significance and Clinicopathological Characteristics. [Abstract]2022 Jun 21:2022:3276925. PMID: 35774848
Solvente y solubilidad
DMSO : 10 mg/mL (34.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.44 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
In brief, cells are treated with WZ811 at 37°C for 24 h. After collection and washing with phosphate-buffered saline (PBS) buffer, cells are resuspended with staining buffer at a final density of 1 × 106/mL. Then, 5 μL annexin V-APC is added to 100 μL cell suspensions and incubated at room temperature in the dark for 10 min. Finally, cells are analyzed with FACS Calibur to determine cell apoptosis profiles[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
A total of 1 × 106 TF-1 cells in 100 μL of PBS are injected subcutaneously into dorsal flanks of an immunodeficient nude mouse. The animals are treated with WZ811 (40 mg/kg), or WZ811 once daily by oral gavage once the tumors have reached 100 mm3. Tumor growth and body weight is measured every three days during the treatment. The tumor volume (TV) is calculated every 3 days according to the following standard formula: TV (mm3) = length × width2 × 0.5[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4440 mL | 17.2200 mL | 34.4400 mL | 86.1000 mL |
| 5 mM | 0.6888 mL | 3.4440 mL | 6.8880 mL | 17.2200 mL | |
| 10 mM | 0.3444 mL | 1.7220 mL | 3.4440 mL | 8.6100 mL | |
| 15 mM | 0.2296 mL | 1.1480 mL | 2.2960 mL | 5.7400 mL | |
| 20 mM | 0.1722 mL | 0.8610 mL | 1.7220 mL | 4.3050 mL | |
| 25 mM | 0.1378 mL | 0.6888 mL | 1.3776 mL | 3.4440 mL | |
| 30 mM | 0.1148 mL | 0.5740 mL | 1.1480 mL | 2.8700 mL |
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