Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 是一种有效的，选择性的，可口服的 CXCR4 拮抗剂，能够拮抗 125I-SDF 与 CXCR4 结合，IC50 值为 13 nM；Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 能够抑制 HIV-1 (NL4.3 strain) 的复制，在 MT-4 和 PBMCs 细胞中，IC50 值分别为 1 和 9 nM。
货号:ajcx13994
CAS:2309699-17-8
分子式:C21H30Cl3N5
分子量：458.86
溶解度:DMSO: 6 mg/mL (13.08 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.