1G,10G,100G,1KG
| 中文名称 | 1G,10G,100G,1KG |
|---|---|
| 中文同义词 | N-[[4-(1,4,8,11-四氮杂环十四烷-1-基甲基)苯基]甲基]-2-吡啶甲胺 |
| 英文名称 | AMD 3465 |
| 英文同义词 | 1G,10G,100G,1KG;N-[[4-(1,4,8,11-Tetraazacyclotetradec-1-ylmethyl)phenyl]methyl]-2-pyridinemethanamine;2-Pyridinemethanamine, N-[[4-(1,4,8,11-tetraazacyclotetradec-1-ylmethyl)phenyl]methyl]- |
| CAS号 | 185991-24-6 |
| 分子式 | C24H38N6 |
| 分子量 | 410.6 |
| EINECS号 | |
| 相关类别 | 小分子药物 |
| Mol文件 | 185991-24-6.mol |
| 结构式 |  |
1G,10G,100G,1KG 性质
| 熔点 | 200-205 °C (decomp) |
|---|---|
| 沸点 | 571.3±50.0 °C(Predicted) |
| 密度 | 1.022±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 10.30±0.20(Predicted) |
| 颜色 | 米白色至浅黄色 |
|
12G5 mAb-CXCR4 0.75 nM (IC 50 , in SupT1 cells) |
CXCL12 AF647 -CXCR4 18 nM (IC 50 , in SupT1 cells) |
X4 HIV-1 (III B ) 12.3 nM (IC 50 , in MT-4 cells) |
X4 HIV-1 (NL4.3) 6.1 nM (IC 50 , in MT-4 cells) |
X4 HIV-1 (NL4.3 AMD3100 ) 2822 nM (IC 50 , in MT-4 cells) |
X4 HIV-1 (RF) 7.4 nM (IC 50 , in MT-4 cells) |
X4 HIV-1 (HE) 9.8 nM (IC 50 , in MT-4 cells) |
HIV-2 (ROD) 12.3 nM (IC 50 , in MT-4 cells) |
HIV-2 (EHO) 12.3 nM (IC 50 , in MT-4 cells) |
AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC 50 s of 0.75 nM and 18 nM in SupT1 cells. AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC 50 of 17 nM, 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 (IC 50 : 1-10 nM), 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 IC 50 ranging from 6 to 12 nM. The IC 50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM. 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.
AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts.