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