| Description | Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 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 (IC50s: 1 and 9 nM). |
| In vitro | Mavorixafor (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2) [1]. Mavorixafor (6.6 μM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells [2]. |
| In vivo | Mavorixafor (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]. |
| Target activity | HIV-1 (NL4.3 strain):9 nM (in PBMCs), HIV-1:26 nM (IC90, in PBMCs), HIV-1 (NL4.3 strain):1 nM (in MT-4 cells), HIV-1 (NL4.3 strain):3 nM (IC90, in MT-4 cells), [125I]-SDF-CXCR4:13 nM |
| Synonyms | AMD-070 trihydrochloride |
| molecular weight | 458.86 |
| Molecular formula | C21H30Cl3N5 |
| CAS | 2309699-17-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 6 mg/mL (13.08 mM), Sonication is recommended. |
| 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. 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. |
Mavorixafor trihydrochloride
CAS No.: 2309699-17-8
Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF bi
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