WZ811

Names

[ Name ]:
WZ811

[Synonym ]:
1,4-Benzenedimethanamine, N,N-di-2-pyridinyl-
N,N'-[1,4-Phenylenebis(methylene)]di(2-pyridinamine)
cc-645
N1,N4-di-2-Pyridinyl-1,4-benzenedimethanamine
WZ811
N,N'-(benzene-1,4-diyldimethanediyl)dipyridin-2-amine
WZ 811

Biological Activity

[Description]:

WZ811 is a potent CXCR4 antagonist, effectively inhibits TN14003 binding to CXCR4, with an EC50 of 0.3 nM.

[Related Catalog]:

Research Areas >> Cancer

[Target]

TN14003-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. WZ811 also suppresses CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cyclic adenosine monophophate (cAMP) levels (EC50, 1.2 nM) and SDF-1 induced Matrigel invasion (EC50, 5.2 nM)[1]. WZ811 (1, 5, 10, 20, 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].

[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].

[Cell Assay]

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].

[Animal admin]

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].

[References]

[1]. WZ811, et al. Discovery of small molecule CXCR4 antagonists. J Med Chem. 2007 Nov 15;50(23):5655-64.

[2]. Li SH, et al. Suppression of chronic lymphocytic leukemia progression by CXCR4 inhibitor WZ811. Am J Transl Res. 2016 Sep 15;8(9):3812-3821.

[Related Small Molecules]

Reparixin | AMG 487 | SCH 527123 | SB 225002 | AZD-5069 | LY2510924 | SCH 546738 | TAK-779 | BKT140 acetate salt | Danirixin | AZD8797 | Baohuoside I | SCH 563705 | IT1t dihydrochloride

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
493.2±35.0 °C at 760 mmHg

[ Melting Point ]:
192-194℃ (methanol )

[ Molecular Formula ]:
C₁₈H₁₈N₄

[ Molecular Weight ]:
290.362

[ Flash Point ]:
252.1±25.9 °C

[ Exact Mass ]:
290.153137

[ PSA ]:
49.84000

[ LogP ]:
2.99

[ Appearance of Characters ]:
white to tan

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.693

[ Storage condition ]:
Store at -20°C

[ Water Solubility ]:
DMSO: ≥7mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-36/37/38

[ Safety Phrases ]:
26

[ RIDADR ]:
NONH for all modes of transport

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