AMD 3465
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| 包装规格: | 1mg 5mg 10mg 25mg 50mg 100mg in glass bottle |
| 产品简介: | 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: | 12G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 cells);CXCL12AF647-CXCR4:18 nM (IC50, in SupT1 cells);X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells);X4 HIV-1 (NL4.3):6.1 nM (IC50, in MT-4 cells);X4 HIV-1 (NL4.3AMD3100):2822 nM (IC50, in MT-4 cells);X4 HIV-1 (RF):7.4 nM (IC50, in MT-4 cells);X4 HIV-1 (HE):9.8 nM (IC50, in MT-4 cells);HIV-2 (ROD):12.3 nM (IC50, in MT-4 cells);HIV-2 (EHO):12.3 nM (IC50, in MT-4 cells) |
| 体外研究: | AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells. AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 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 (IC50: 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 IC50 ranging from 6 to 12 nM. The IC50 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. |
| 体内研究: | AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts. |
| 保存条件: | -20℃ |
| 注意事项: | 1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。 |
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