Uses
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome[1].
in vivo
Mavorixafor (AMD-070) (2 mg/kg, p.o.) significantly reduces the number of metastatic lung nodules in mice, and lowers the expression of human Alu DNA in mice, without body weight loss[2].
IC 50
125I-SDF-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)
References
[1] Skerlj RT, et al. Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. J Med Chem. 2010 Apr 22;53(8):3376-88. DOI:
10.1021/jm100073m[2] Uchida D, et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells. Oncol Rep. 2018 Jul;40(1):303-308. DOI:
10.3892/or.2018.6400
