AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively).

AMG487 blocked in vitro lymphocyte migration mediated by CXCL9, CXCL10 or CXCL11. AMG487 did not affect the proliferation of 66.1 tumor cells at 24, 48 or 72 hours under normal or serum-free growth conditions. It did inhibit the migration of the tumor cells to CXCL9 by 70% [3].

AMG487 displayed an inhibitory effect on experimental lung metastasis. Treatment with bleomycin via intra-tracheal installation after tracheostomy induced cellular recruitment into the lungs in the lungs of mice. All but the lowest dose AMG 487 treatment group showed a significant reduction in cellular infiltration into the lungs (p < 0.005 as determined by Student’s t-test). Subcutaneously administration with AMG 487 (3 mg/kg, twice daily) showed migration inhibition results similar to those of CXCR3 deficient mice (n = 8-12 mice per group). The highly malignant murine mammary tumor cell line 66.1 was pretreated with AMG 487 and hence i.v. injected into immune-competent female mice [2][3].