| 产品描述： | AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) 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 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses. |
| 靶点： |
12G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 cells);CXCL12AF647-CXCR4:18 nM (IC50, in SupT1 cells);X4 HIV-1 (NL4.3):6.1 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);X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells);X4 HIV-1 (NL4.3AMD3100):2822 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);HIVProtease |
| 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 |
| 参考文献： |
1. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. 2. Yang L, et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res. 2007 Jan 15;67(2):651-8. |
| 溶解性： |
DMSO : 50 mg/mL (55.80 mM; Need ultrasonic) H2O : ≥ 38 mg/mL (42.41 mM) |
| 保存条件： |
2-8℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.116 ml |
5.58 ml |
11.16 ml |
| 5 mM |
0.223 ml |
1.116 ml |
2.232 ml |
| 10 mM |
0.112 ml |
0.558 ml |
1.116 ml |
| 50 mM |
0.022 ml |
0.112 ml |
0.223 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京