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WZ811 {[allProObj[0].p_purity_real_show]}

货号:A220173

WZ811 is a small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.

WZ811 化学结构 CAS号:55778-02-4
WZ811 化学结构
CAS号:55778-02-4
WZ811 3D分子结构
CAS号:55778-02-4
WZ811 化学结构 CAS号:55778-02-4
WZ811 3D分子结构 CAS号:55778-02-4
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WZ811 纯度/质量文件 产品仅供科研

货号:A220173 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CXCR1 CXCR2 CXCR4 其他靶点 纯度
Reparixin 99%+
SB225002 +++

CXCR2, IC50: 22 nM

99%+
Plerixafor ++

CXCR4, IC50: 44 nM

99%
AMD 3465 6HBr 98%
WZ811 ++++

CXCR4, EC50: 0.3 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

WZ811 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]

WZ811 动物研究

Dose Mice: 4 mg/kg[3] (i.g.), 40 mg/kg[2] (p.o.)
Administration i.g., p.o.

WZ811 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.

WZ811 实验方案

计算器
存储液制备 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

WZ811 技术信息

CAS号55778-02-4
分子式C18H18N4
分子量 290.362
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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