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AMD 3465 hexahydrobromide

Cat. No.:YN321050

  • CAS No. :185991-07-5

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    • 产品名称: AMD 3465 hexahydrobromide
      CAS No.: 185991-07-5
      Chemical Name: N-[[4-(1,4,8,11-tetraazacyclotetradec-1-ylmethyl)phenyl]methyl]-2-pyridinemethanamine, hexahydrobromide
      Synonyms:GENZ-644494 hexahydrobromide
      分子量:896.07
      分子式:C₂₄H₄₄Br₆N₆
      SMILES:[H]Br.[H]Br.[H]Br.[H]Br.[H]Br.[H]Br.C1(CNCC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)=NC=CC=C1
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) 是一种有效的CXCR4拮抗剂,在 SupT1 细胞中,能够抑制 12G5 mAb,CXCL12AF647与CXCR4的结合,IC50值分别为 0.75 nM 和 18 nM;AMD 3465 同时可有效抑制X4 HIV的复制 (IC50,1-10 nM),但对 R5 HIV 病毒无作用。
      IC50和靶点: [{name:"12G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 cells)"},{name: "CXCL12AF647-CXCR4:18 nM (IC50, in SupT1 cells)"},{name: "X4 HIV-1 (NL4.3):6.1 nM (IC50, in MT-4 cells)"},{name: "X4 HIV-1 (RF):7.4 nM (IC50, in MT-4 cells)"},{name: "X4 HIV-1 (HE):9.8 nM (IC50, in MT-4 cells)"},{name: "X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells)"},{name: "X4 HIV-1 (NL4.3AMD3100):2822 nM (IC50, in MT-4 cells)"},{name: "HIV-2 (ROD):12.3 nM (IC50, in MT-4 cells)"},{name: "HIV-2 (EHO):12.3 nM (IC50, in MT-4 cells)"}]
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    • Broxmeyer, H.E., Orschell, C.M., Clapp, D.W., et al.Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonistJ. Exp. Med.201(8),1307-1318(2005)

      Dorsam, R.T., and Gutkind, J.S.G-protein-coupled receptors and cancerNat. Rev. Cancer7(2),79-94(2007)

      Tamamura, H., Hiramatsu, K., Ueda, S., et al.Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131J. Med. Chem.48(2),380-391(2005)

      Hatse, S., Princen, K., De Clercq, E., et al.AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitorBiochem. Pharmacol.70,752-761(2005)

      Hu, J.S., Freeman, C.M., Stolberg, V.R., et al.AMD3465, a novel CXCR4 receptor antagonist, abrogates schistosomal antigen-elicited (type-2) pulmonary granuloma formationAm. J. Pathol.169(2),424-432(2006)

      Yang, L., Jackson, E., Woerner, B.M., et al.Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivoCancer Res.67(2),651-658(2007)

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