Mavorixafor (AMD-070, AMD-11070) is a potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.
AMD-070 displays no significant activity (IC50>10 uM) for a series of other closely GPCRs (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2).
AMD-070 inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with IC50 of 2 nM and 26 nM, respectively, with noncytotoxic to cells (>23 uM).
AMD-070 exhibits good PK profiles and excellent oral bioavailability.
AMD-070 also inhibits CXCR4/SDF-1-mediated events in ALL cancer cells and transplant models.
