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.

AMD3465 is a highly selective chemokine receptor CXCR4 antagonist with antiviral and anticancer activity. The chemokine receptor CXCR4 is expressed on a wide variety of leukocytes and is the predominant receptor for stromal cell-derived factor-1 (SDF1, CXCL12) in addition to acting as a co-receptor for HIV entry into cells. AMD3465 blocks surface binding of CXCL12 (SDF-1α). AMD3465 is an antagonist of SDF-1 ligand binding (K(i) of 41.7+/-1.2 nM). AMD3465 was found to halt the progression of an agressive childhood blood cancer, T-cell acute lymphoblastic leukemia (T-ALL), within two weeks of starting treatment in an animal model.

Packaging

5, 25 mg in glass bottle