Mavorixafor trihydrochloride (Synonyms: AMD-070 trihydrochloride) |
| Catalog No.GC36550 |
El trihidrocloruro de mavorixafor (trihidrocloruro de AMD-070) es un antagonista de CXCR4 potente, selectivo y disponible por vÍa oral, con un valor IC50 de 13 nM frente a la uniÓn de CXCR4 125I-SDF, y también inhibe la replicaciÓn de T-tropic HIV-1 (cepa NL4.3 ) en células MT-4 y PBMC con una IC50 de 1 y 9 nM, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2309699-17-8
Sample solution is provided at 25 µL, 10mM.
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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. 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)
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].
[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.
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