中文名称: AMD 3465
英文名称: AMD 3465
CAS No: 185991-24-6
分子式: C24H38N6
分子量: 410.6
A11456 AMD 3465 (psaitong)
包装规格:
1mg in glass bottle
产品描述:

基本信息

产品编号:

A11456

产品名称:

AMD 3465

CAS:

185991-24-6

 

储存条件

粉末

-20℃

四年

分子式:

C24H38N6

溶于液体

-80℃

二年

分子量:

410.60

 

 

化学名: 

1G,10G,100G,1KG  N-[[4-(1,4,8,11-tetraazacyclotetradec-1-ylmethyl)phenyl]methyl]-2-Pyridinemethanamine

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

生物活性

产品描述

一种有效的CXCR4拮抗剂,在SupT1细胞中,能够抑制12G5 mAb,CXCL12AF647与CXCR4结合,IC50值分别为0.75nM和18nM;AMD 3465同时可有效抑制X4 HIV的复制(IC50,1-10nM)但对R5 HIV病毒无作用。

靶点

CXCR

HIV

 

体外研究

AMD 3465 is a potent antagonist of CXCR4,inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4,with IC50s of 0.75nM and 18nM in SupT1 cells.AMD 3465 (50nM) totally blocks CXCL12-induced calcium mobilization,with an IC50 of 17nM,but shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES,LD78β and MIP-1β in U87.CD4.CCR5 cells.AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50:1-10nM),but has no effect on CCR5-using (R5) viruses.AMD3465 is cytotoxic to the X4 HIV-1 strains IIIB,NL4.3,RF and HE with an IC50 ranging from 6 to 12nM.The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3nM.AMD 3465 inhibits CXCL-12-induced growth in U87 and Daoy cells.AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells.

体内研究

AMD 3465 (2.5mg/kg/d,s.c.for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts.

 

推荐实验方法(仅供参考)

细胞实验:

 

Following serum starvation for 24h,astrocytes, granule cells,U87 cells,and Daoy cells are treated with 1μg/mL CXCL12,2.5ng/mL AMD 3465,200μM rolipram,or 10μM forskolin.Daoy and U87 cell growth in culture is measured by trypan blue exclusion after 24 and 48h of treatment,respectively.MCE has not independently confirmed the accuracy of the

 

动物实验:

 

Mice

Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates.Two weeks after tumor cell implantation,cohorts of mice with approximately equivalent tumor bioluminescence are divided into equal control and treatment groups.Animals in AMD 3465 experiments receive s.c.osmotic pumps loaded with 10mg/mL AMD 3465 in sterile PBS or PBS alone.The infusion rate is 0.25μL/h (50μg/d).For the experiments with rolipram or caffeine,mice in the treatment groups receive oral administration of rolipram (5μg/g/d) or caffeine (100μg/g/d).The concentration of drug in the water is determined from daily measurements of water consumption by each animal over the course of 7 days.Concentrations are adjusted based on water consumption to provide the prescribed dose.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
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摩尔浓度计算公式

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开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):