1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. WZ811

WZ811 

Cat. No.: HY-15478 Purity: ≥99.0%
Handling Instructions

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).

For research use only. We do not sell to patients.

WZ811 Chemical Structure

WZ811 Chemical Structure

CAS No. : 55778-02-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 225 In-stock
Estimated Time of Arrival: December 31
100 mg USD 315 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

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)[1].

IC50 & Target[1]

CXCR4

0.3 nM (EC50)

In Vitro

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].

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

In Vivo

WZ811 (40 mg/kg, p.o.) blocks the lymphocytic leukemia cells growth on mouse xenograft models, and inhibits CXCR4/PI3K/AKT signaling pathway in mouse xenograft model of lymphocytic leukemia[2].

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

Molecular Weight

290.36

Formula

C₁₈H₁₈N₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (34.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4440 mL 17.2200 mL 34.4400 mL
5 mM 0.6888 mL 3.4440 mL 6.8880 mL
10 mM 0.3444 mL 1.7220 mL 3.4440 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (3.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (3.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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].

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

Animal Administration
[2]

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].

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

References

Purity: ≥99.0%

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WZ811
Cat. No.:
HY-15478
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