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WZ811

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Chemical Structure| 55778-02-4 同义名 : -
CAS号 : 55778-02-4
货号 : A220173
分子式 : C18H18N4
纯度 : 98%
分子量 : 290.362
MDL号 : MFCD18086914
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CXCR4

    CXCR4, EC50:0.3 nM
描述 Through binding with CC- and CXC-chemokines, CCR and CXCR, the subsets of the chemokine receptor family can trigger an intracellular signal transduction cascade, thus mediating the recruitment of immune cells to the inflammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. WZ811 is a potent and selective CXCR4 inhibitor with subnanomolar EC50 value of 0.3nM. Pre-treatment with WZ811 for 15min dose-dependently caused reduction of SDF-1 (150ng/ml)-induced cAMP level with EC50 of 1.2nM (measured by TR-FRET based LANCE assay kit). The inhibition of SDF-1 induced matrigel invasion by WZ811 can also be observed with EC50 of 5.2nM[1]. Treatment with WZ811 for 48h at dose ranging in 5-40μM significantly inhibited proliferation of chronic lymphocytic leukemia cells, TF-1 and UT-7, as well as induced apoptosis at dose of 5μM for 24h. Daily oral dose with WZ811 (40mg/kg) for 25days suppressed the lymphocytic leukemia cells growth on mouse xenograft models[2].
作用机制 WZ811 can inhibit CXCR4 through the competition binding.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.44mL

0.69mL

0.34mL

17.22mL

3.44mL

1.72mL

34.44mL

6.89mL

3.44mL
参考文献

[1]Zhan W, Liang Z, et al. Discovery of small molecule CXCR4 antagonists. J Med Chem. 2007 Nov 15;50(23):5655-64. Epub 2007 Oct 24.

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