WZ811

Modify Date: 2024-01-02 23:29:02

WZ811 Structure
WZ811 structure
Common Name WZ811
CAS Number 55778-02-4 Molecular Weight 290.362
Density 1.2±0.1 g/cm3 Boiling Point 493.2±35.0 °C at 760 mmHg
Molecular Formula C18H18N4 Melting Point 192-194℃ (methanol )
MSDS Chinese USA Flash Point 252.1±25.9 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of WZ811


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

 Names

Name N-[[4-[(pyridin-2-ylamino)methyl]phenyl]methyl]pyridin-2-amine
Synonym More Synonyms

 WZ811 Biological Activity

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

 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

 Safety Information

Symbol GHS07
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

 Articles1

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 Synonyms

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
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