製品の概要

  • 製品名

    AMD3100 octahydrochloride, CXCR4 antagonist
  • 製品の詳細

    Highly selective CXCR4 antagonist
  • 別名

    • AMD 3100
    • JM 3100
    • Mobozil
    • SID 791
  • 生理活性の詳細

    Plerixafor (hydrochloride) is a macrocyclic compound that acts as an irreversible antagonist against the binding of CXCR4 with its ligand, SDF-1 (CXCL12).


    It suppresses infection by HIV with an IC50 value of 1-10 ng/ml with selectivity toward CXCR4-tropic virus. Plerixafor mobilizes hematopoietic stem and progenitor cells for transplant better than G-CSF alone. It also increases T-cell trafficking in the blood and spleen as well as the central nervous system. Plerixafor regulates the growth of primary and metastic breast cancer cells and inhibits dissemination of ovarian carcinoma cells.

  • 精製度

    > 99%
  • CAS 番号

    155148-31-5
  • 構造式

    Chemical Structure

製品の特性

画像

  • Uninfected control DCs were treated with MeAIB, MSO, inhibitors of CXCR4 (AMD3100), PI3K (LY294002) or Rho kinase (Y27632), or Gln starvation for 2 hours before assessing migration to 100 ng/ml SDF-1 α. Chemotactic index (CI) is defined as the fold increase in the number of migrating DCs to SDF-1 α over the spontaneous migration. One-way ANOVA reveals an effect of pharmacological treatments on the SDF-1 α-induced migration (F(6,44) = 6.700, P<0.001). Asterisks indicate P<0.05 (Dunnett's post hoc).

参考文献

This product has been referenced in:

  • De Clercq E The AMD3100 story: the path to the discovery of a stem cell mobilizer (Mozobil). Biochem Pharmacol 77:1655-64 (2009). Read more (PubMed: 19161986) »
  • Rusconi S  et al. New macrocyclic amines showing activity as HIV entry inhibitors against wild type and multi-drug resistant viruses. Molecules 14:1927-37 (2009). Read more (PubMed: 19471212) »
  • Fransen S  et al. Suppression of dualtropic human immunodeficiency virus type 1 by the CXCR4 antagonist AMD3100 is associated with efficiency of CXCR4 use and baseline virus composition. Antimicrob Agents Chemother 52:2608-15 (2008). Read more (PubMed: 18443125) »
  • Fricker SP  et al. Characterization of the molecular pharmacology of AMD3100: a specific antagonist of the G-protein coupled chemokine receptor, CXCR4. Biochem Pharmacol 72:588-96 (2006). Read more (PubMed: 16815309) »
  • Broxmeyer HE  et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med 201:1307-18 (2005). Read more (PubMed: 15837815) »
  • De Clercq E  et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob Agents Chemother 38:668-74 (1994). Read more (PubMed: 7913308) »
See all 8 Publications for this product

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