Uses
AMD 3465 is a CXCR4 antagonist and in combination with monoclonal antibody, was shown to be potentially effective in reducing tumor growth and increasing survival in patient with B cell lymphoma
Biochem/physiol Actions
AMD3465 is also termed as{N-[1,4,8,11-tetraazacyclotetradecanyl-1,4-phenylenebis(methylene)]-2-(aminomethyl)pyridine}. It controls oncogenic signaling and invasiveness in vitro. It inhibits breast cancer growth and metastasis in vivo. As a chemokine receptor 4 (CXCR4) antagonist, AMD3465 is ten times more efficient than bicyclam AMD3100.
in vivo
AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts[2].
IC 50
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)
