mRNA synthesis In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail Tyramide Signal Amplification (TSA) TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc. Phos Binding Reagent Acrylamide Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody Cell Counting Kit-8 (CCK-8) A convenient and sensitive way for cell proliferation assay and cytotoxicity assay SYBR Safe DNA Gel Stain Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels. Inhibitor Cocktails Protect the integrity of proteins from multiple proteases and phosphatases for different applications. BackgroundChemical Properties试验操作质量控制BackgroundAMD-070是一种选择性的、具有口服生物利用度的趋化因子受体CXCR4拮抗剂，IC50值为13 nM [1]。CXCR4是在肿瘤发展中起着重要作用的G蛋白偶联受体。它通过CXCL12介导的MAPK信号转导来影响肿瘤细胞的迁移、增殖和存活。AMD-070是一种具有口服生物利用度的CXCR4拮抗剂，研究发现它是肿瘤细胞迁移的抑制剂。CXCR4也是两个趋化因子受体（被病毒用于感染人类细胞）的其中之一。作为CXCR4抑制剂，AMD-070能够强效抑制X4型(T嗜性) HIV-1复制及gp120/CXCR4的相互作用。机制研究表明AMD-070是一种变构抑制剂。研究发现，AMD-070的苯并咪唑与CXCR4的Tyr残基之间形成了一个氢键，而Asp262、Asp171和Glu288残基没有与AMD-070发生直接相互作用[1、2及3]。AMD-070对CXCR4而非其他相关G蛋白偶联趋化因子受体（包括CXCR1、 CXCR2、 CCR1、CCR2b、CCR4及CCR5）有选择性。AMD-070对这些GPCRs的IC50值都高于10 μM。在表达人CXCR4的HOS细胞中，AMD-070抑制HIV-1感染，IC50值为10 nM。在CD4+CXCR4+T细胞中，AMD-070通过抑制SDF-1诱导的钙流（IC50值为12 nM），具有抗艾滋病病毒（HIV-1）活性。此外，AMD-070抑制125I-SDF-1的竞争性结合，IC50值为13 nM。在黑色素瘤细胞CHL-1和A375中，AMD-070用药显著抑制细胞迁移。另外，该抑制剂还可增加细胞空隙大小[1，2，4]。参考文献：[1] Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D, Wilson T, Harwig C, Hatse S, Princen K, De Clercq E, Schols D. 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] O\'Boyle G, Swidenbank I, Marshall H, Barker CE, Armstrong J, White SA, Fricker SP, Plummer R, Wright M, Lovat PE. Inhibition of CXCR4-CXCL12 chemotaxis in melanoma by AMD11070. Br J Cancer. 2013 Apr 30;108(8):1634-40. [3] Wong RS, Bodart V, Metz M, Labrecque J, Bridger G, Fricker SP. Comparison of the potential multiple binding modes of bicyclam, monocylam, and noncyclam small-molecule CXC chemokine receptor 4 inhibitors. Mol Pharmacol. 2008 Dec;74(6):1485-95. [4] Gudmundsson KS, Sebahar PR, Richardson LD, Miller JF, Turner EM, Catalano JG, Spaltenstein A, Lawrence W, Thomson M, Jenkinson S. Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5048-52.Chemical PropertiesPhysical AppearanceA brown oilStorageStore at -20°CM.Wt349.48Cas No.558447-26-0FormulaC21H27N5SynonymsAMD 070; AMD070Solubility≥17.45 mg/mL in DMSO; ≥44.5 mg/mL in EtOH; ≥7.47 mg/mL in H2O with gentle warmingChemical NameN\'-(1H-benzimidazol-2-ylmethyl)-N\'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamineSDFDownload SDFCanonical SMILESC1CC(C2=C(C1)C=CC=N2)N(CCCCN)CC3=NC4=CC=CC=C4N3运输条件 蓝冰运输或根据您的需求运输。一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。试验操作该化合物在DMSO中的溶解度大于17.5mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。在黑色素瘤细胞CHL-1和A375中，AMD-070的治疗显著抑制细胞迁移。此外，抑制剂处理也增加了细胞的空隙大小。在表达人CXCR4的HOS细胞中，AMD-070抑制HIV-1感染，IC50值为10 nM。由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。References:[1] O\'boyle G, Swidenbank I, Marshall H, et al. Inhibition of CXCR4–CXCL12 chemotaxis in melanoma by AMD11070[J]. British journal of cancer, 2013, 108(8): 1634.[2] Gudmundsson K S, Sebahar P R, Richardson L D A, et al. Amine substituted N-(1H-benzimidazol-2ylmethyl)-5, 6, 7, 8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1[J]. Bioorganic & medicinal chemistry letters, 2009, 19(17): 5048-5052.Apexbio 中国电话: 021-55669583传真: 021-55669583 电子邮箱: sales@apexbio.cn