MavorixaforMavorixafor
MedChemExpress (MCE)
HY-50101
558447-26-0
AMD-070
AMD-11070
4°C, stored under nitrogen *In solvent : -80°C, 6 months
-20°C, 1 month (stored under nitrogen)
Room temperature in continental US
may vary elsewhere.
Mavorixafor (AMD-070) 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 can be used for the study of WHIM syndrome.
Mavorixafor (AMD-070) is a potent 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 (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2)[1]. Mavorixafor (AMD-070) (6.6 μM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells[2].
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].
Mice[2] BALB/c nude mice are maintained under pathogen-free conditions. The experiments are initiated when the mice are 8 weeks of age. Briefly, the cells are inoculated into the blood vessels of nude mice (1× 106). These mice are sacrificed at day 49. The presence or absence of distant metastases is confirmed by hematoxylin and eosin (H&E) staining. For experimental chemotherapy, the mice are treated by the daily oral administration of 0.2 mL of saline for a vehicle or the same volume of Mavorixafor (AMD-070) (2 mg/kg)[2].
Cells are seeded on a 96-well plate at 5 × 103 cells/well in DMEM containing 10% FCS. Twenty-four hours later, the cells are treated with or without 2 µM AMD3100 or 6.6 µM AMD-070. After 24 or 48 h, the number of cells is quantified by an assay using MTT[2].
125I-SDF-CXCR4 13 nM (IC50) HIV-1 (NL4.3 strain) 1 nM (IC50, in MT-4 cells) HIV-1 (NL4.3 strain) 9 nM (IC50, in PBMCs) HIV-1 (NL4.3 strain) 3 nM (IC90, in MT-4 cells) HIV-1 (NL4.3 strain) 26 nM (IC90, in PBMCs)
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[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. [Content Brief]
[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. [Content Brief]