Uses
N-(1H-Benzimidazol-2-ylmethyl)-N-[(8S)-5,6,7,8-tetrahydro-8-quinolinyl]-1,4-butanediamine Monohydrochloride is a potent and selective antagonist of CXCR4. It is also an inhibitor of X4-tropic HIV virus.
Biological Activity
AMD070 (AMD11070) is an orally active, reversible and selective CXCR4 (CD184, fusin) antagonist (IC50 = 13 nM against 100 pM 125I-SDF-1α for binding human CD+/CXCR4+ CEM-CCRF cells) th at inhibits HIV-1 replication in cultures (IC50/host cells = 2 nM/MT-4 and 26 nM/PBMCs; T-tropic HIV-1NL4.3 strain) with no host cytotoxicity even at concentrations above 23 μM.
in vivo
Mavorixafor (2 mg/kg; po; once a day; for 49 days) hydrochloride significantly inhibits the lung metastasis of B88 SDF 1 cells in nude mice[2].
| Animal Model: | BALB/c nude mice (8 weeks of age) injected with B88-SDF-1 cells[2] |
| Dosage: | 2 mg/kg |
| Administration: | Oral administration; once a day; for 49 days |
| Result: | A significant reduction in the number of metastatic lung nodules was observed in the mice. |
IC 50
125I-CXCL12-CXCR4: 13 nM (IC
50); HIV-1 (NL4.3 strain): 1 nM (IC
50, In MT-4 cells); HIV-1 (NL4.3 strain): 9 nM (IC
50, In PBMCs); HIV-1 (NL4.3 strain): 3 nM (IC90, In MT-4 cells); HIV-1 (NL4.3 strain): 26 nM (IC90, In PBMCs)
