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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC 50 value of 13 nM against CXCR4 125 I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC 50 of 1 and 9 nM, respectively.
In Vitro
Mavorixafor (AMD-070) is a potent and orally available CXCR4 antagonist, with an IC 50 value of 13 nM against CXCR4 125 I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC 50 of 1 and 9 nM, respectively. Mavorixafor (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2). Mavorixafor (AMD-070) (6.6 µM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
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 Mavorixafor (AMD-070) or 6.6 µM AMD-070 . After 24 or 48 h , the number of cells is quantified by an assay using MTT. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Mice 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 Mavorixafor (AMD-070) (2 mg/kg) . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:125 I-SDF-CXCR4 13 nM (IC 50 ) HIV-1 (NL4.3 strain) 1 nM (IC 50 , in MT-4 cells) HIV-1 (NL4.3 strain) 9 nM (IC 50 , in PBMCs) HIV-1 (NL4.3 strain) 3 nM (IC90, in MT-4 cells) HIV-1 (NL4.3 strain) 26 nM (IC90, in PBMCs)
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 有机杂环化合物 |
| 类(Class) | 喹啉及其衍生物 |
| 亚类(Subclass) | 氨基喹啉及其衍生物 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 氨基喹啉及其衍生物 |
| 其他上位类(Alternative Parents) | 氢化喹啉 苯并咪唑类 芳烷基胺 吡啶及其衍生物 苯类化合物 咪唑类 杂芳族化合物 三烷基胺 氮杂环化合物 单烷基胺 盐酸盐 碳氢化合物衍生物 |
| 分子骨架(Molecular Framework) | 芳香族杂多环化合物 |
| 取代基(Substituents) | 氨基酸 - 氨基吡啶 - 芳烷基胺 - 芳香族杂多环化合物 - 氮杂环 - 吡唑 - 苯基化合物 - 苯并咪唑 - 杂芳香族化合物 - 烃衍生物 - 氟氯烃 - 咪唑 - 有机硝基化合物 - 有机氮化合物 - 初级脂肪胺 - 初级胺 - 吡啶 - 三元脂肪胺 - 三芳基胺 - 四氢喹啉 |
| 描述(Description) | 该化合物属于有机化合物中的氨基喹啉及其衍生物类。该类化合物含有连接于喹啉环系的氨基。 |
| 外部描述符(External Descriptors) | 暂无 |