化合物AMD-070 TQ0174

Product Introduction
Bioactivity


英文名: Mavorixafor

描述: Mavorixafor (AMD-070) 是一种有效的特异性 CXCR4 拮抗剂，对 CXCR4 125I-SDF 结合的 IC50 值为 13 nM。 Mavorixafor 在 MT-4 细胞 (IC50 = 1 nM) 和 PBMC (IC50 = 9 nM) 中抑制 T-tropic HIV-1 (NL4.3 株) 的复制。

细胞实验: Cells are seeded on a 96-well plate at 5 × 10^3 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].

动物实验: 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× 10^6). 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 AMD-070 (2 mg/kg) [2].

体外活性: Mavorixafor (6.6 µM) 显著降低了B88-SDF-1细胞的锚定依赖性生长、迁移和Matrigel侵袭[1]。Mavorixafor 对其他趋化因子受体（CCR1、CCR2b、CCR4、CCR5、CXCR1和CXCR2）无影响[2]。

体内活性: AMD-070 (2 mg/kg，p.o.) 在小鼠中显著减少了肺转移结节的数量，并降低了小鼠体内人源Alu DNA的表达，而不引起体重减轻[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 44 mg/mL (125.9 mM)
H2O : 7 mg/mL (20.03 mM)
DMSO : 17 mg/mL (48.64 mM)


关键字: CXCR | Mavorixafor | Human immunodeficiency virus | AMD070 | HIV | inhibit | CXC chemokine receptors | AMD 070 | Inhibitor

相关产品: Reparixin | ATI-2341 acetate(1337878-62-2 free base) | ITIC | AMD 3465 hexahydrobromide | CXCR4-IN-2 | ITIC-4F | Baohuoside I | Motixafortide | CXCR4-IN-1 | AZD8797

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Viral Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途