AMD-070 is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
The G protein-coupled protein receptor C-X-C chemokine receptor 4 (CXCR4) is an attractive target for cancer diagnosis and treatment, as it is overexpressed in many solid and hematologic cancers[1]. Mavorixafor 3HCl represents the first small molecule orally bioavailable CXCR4 antagonist that was developed for the treatment of HIV-1 infection. It is a potent, selective and orally available CXCR4 antagonist with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 2 and 26 nM, respectively, while remaining noncytotoxic to cells at concentrations exceeding 23 μM[2]. Mavorixafor 3HCl at 6.6 µM significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells[3]. The pharmacokinetics of mavorixafor 3HCl was evaluated in rat and dog, and good oral bioavailability was observed in both species[2]. Mavorixafor 3HCl (2 mg/kg, p.o.) significantly reduced the number of metastatic lung nodules in mice, and lowers the expression of human Alu DNA in mice, without body weight loss[3].
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