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CAS No.: 55778-02-4

WZ811 Catalog No. CSN15996

Synonyms: WZ811

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

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CXCR4

EC50:0.3nM
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]
动物研究
剂量
Mice: 4 mg/kg^[3] (i.g.), 40 mg/kg^[2] (p.o.)

给药途径
i.g., p.o.
参考文献

动物研究
剂量	Mice: 4 mg/kg^[3] (i.g.), 40 mg/kg^[2] (p.o.)
给药途径	i.g., p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4440 mL
- 17.2199 mL
- 34.4397 mL
- 5 mM
- 0.6888 mL
- 3.4440 mL
- 6.8879 mL
- 10 mM
- 0.3444 mL
- 1.7220 mL
- 3.4440 mL

技术信息

CAS号

55778-02-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H18N4

运输

蓝冰

分子量

290.36

别名

WZ811

溶解度

DMSO	30.0 mg/mL (103.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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WZ811 Catalog No. CSN15996

靶点选择性

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