生物活性
Plerixafor (AMD3100)是一种CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12调节的趋化性,IC50分别为44 nM和5.7 nM。
化学数据
分子量 |
502.78 |
分子式 |
C28H54N8 |
CAS号 |
110078-46-1 |
纯度 |
99.24% |
溶解性(25°C) |
Ethanol 70 mg/mL Water 2 mg/mL |
储存和运输条件 |
固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
细胞系 |
OS cell lines (LM8 and Dunn) |
方法 |
MTT assay. The effects of CXCL12 and AMD3100 on the survival of two OS cell lines (LM8 and Dunn) were assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at 2×103/well in DMEM-h. After overnight growth, the cells were cultured for 7 days in FBS-free medium in the presence of 0 or 100 ng/ml CXCL12, 30 μM AMD3100 alone or 100 ng/ml CXCL12 with 10, 20 or 30 μM AMD3100. The FBS-free cells without 100 ng/ml CXCL12 or AMD3100 served as the control group. After the 7 day incubation, 20 μl MTT (5 mg/ml; Sigma, St. Louis, MO, USA) was added into each well and incubated for 4 h at 37°C. Culture medium was removed and 150 μl dimethylsulfoxide was added. The optical density (OD) was then measured using a model ELx800 microplate reader (Bio-Tech instruments inc.) at 490 nm. The cell viability was calculated using the equation: Cell viability (%) = (OD490nm of treatment/OD490nm of control) ×100%. |
浓度 |
30 μM |
处理时间 |
7 days |
动物实验 |
动物模型 |
orthotopic animal model of OS in Ten 4-week-old female C3H mice |
配制 |
PBS |
剂量 |
5 mg/kg every 2 days |
给药处理 |
tail vein injection |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
|
小鼠 |
大鼠 |
兔 |
豚鼠 |
仓鼠 |
狗 |
重量 (kg) |
0.02 |
0.15 |
1.8 |
0.4 |
0.08 |
10 |
体表面积 (m2) |
0.007 |
0.025 |
0.15 |
0.05 |
0.02 |
0.5 |
Km系数 |
3 |
6 |
12 |
8 |
5 |
20 |
动物 A (mg/kg) = 动物 B (mg/kg) × |
动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于半岛bd体育手机客户端 分子量,对于特殊半岛bd体育手机客户端 ,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.9889 mL |
9.9447 mL |
19.8894 mL |
5 mM |
0.3978 mL |
1.9889 mL |
3.9779 mL |
10 mM |
0.1989 mL |
0.9945 mL |
1.9889 mL |