WZ811

目录号: GC15989纯度: >98.00%
CXCR4 antagonist

WZ811
Cas No.: 55778-02-4
规格价格库存数量操作
5mg¥377.00现货
1
10mg¥490.00现货
1
25mg¥1,036.00现货
1
50mg¥1,575.00现货
1
100mg¥2,205.00现货
1
200mg¥3,101.00现货
1
10mM (in 1mL DMSO)¥414.00现货
1

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产品描述 Description

WZ811 is a small molecule antagonist of CXC chemokine receptor 4 (CXCR4) [1].

WZ811 is synthesized with two aromatic amine moieties. It is found to effectively inhibit TN14003 binding to CXCR4 with EC50 value of 0.3nM at first. And then WZ811 is found to have ability in counteracting SDF-1 function and blocking CXCR4/SDF-1-mediated signaling. In the cAMP assay, WZ811 reduces the effect on cAMP caused by 150ng/ml SDF-1 significantly. It also blocks the SDF-1 induced Matrigel invasion with EC50 value of 5.2nM. Since CXCR4 is involved in the pathogeneses of a wide range of infectious, inflammatory and other diseases, WZ811 is developed for the treatment of various CXCR4-related diseases. It is reported to have weak anti-HIV activity in cell culture [1, 2].

References:
[1] Zhan W, Liang Z, Zhu A, et al. Discovery of small molecule CXCR4 antagonists. Journal of medicinal chemistry, 2007, 50(23): 5655-5664.
[2] Choi W T, Duggineni S, Xu Y, et al. Drug discovery research targeting the CXC chemokine receptor 4 (CXCR4). Journal of medicinal chemistry, 2011, 55(3): 977-994.

实验参考方法 Experimental Reference Method

Cell experiment:

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 experiment:

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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
55778-02-4
化学名
N-[[4-[(pyridin-2-ylamino)methyl]phenyl]methyl]pyridin-2-amine
SMILES
C1=CC=NC(=C1)NCC2=CC=C(C=C2)CNC3=CC=CC=N3
分子式
C18H18N4
分子量
290.36 g/mol
溶解性
DMF: 3 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol