Catalog Number: 3299
Alternate Names: JM 3100, Plerixafor
Chemical Name: 1,1'-[1,4-Phenylenebis-(methylene)]-bis-(1,4,8,11-tetraazacyclotetradecane) octahydrochloride
Biological Activity
Highly selective CXCR4 chemokine receptor antagonist (IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and all other chemokine receptors respectively). Switches inflammatory responses from Th2 to Th1 type and reduces airway hyperresponsiveness in a mouse model of asthma. Potently inhibits HIV-1 and HIV-2 replication in vitro (EC50 = 4 - 35 nM) and mobilizes hematopoietic stem cells in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water
  • Storage:
    Desiccate at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibits HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker.
    Bridger et al.
    J.Med.Chem., 1995;38:366
  2. The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease.
    Hogaboam et al.
    Pharmacol.Ther., 2005;107:314
  3. Effective mobilization of hematopoietic progenitor cells in G-CSF mobilization defective CD26-/- mice through AMD3100-induced disruption of the CXCL12-CXCR4 axis.
    Paganessi et al.
    Exp.Hematol., 2011;39:384
  4. Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4.
    Hatse et al.
    FEBS Letts., 2002;527:255

The citations listed below are publications that use Tocris products. Selected citations for AMD 3100 octahydrochloride include:

9 Citations: Showing 1 - 9
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  1. Modeling selective elimination of quiescent cancer cells from bone marrow.
    Authors: Cavnar Et al.
    Cell 2015;17:625
  2. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis.
    Authors: Chu Et al.
    Neoplasia 2015;10:e0133616
  3. CXCR4 inhibition ameliorates severe obliterative pulmonary hypertension and accumulation of C-kit+ cells in rats.
    Authors: Farkas Et al.
    PLoS One 2014;9:e89810
  4. Brain glycolipids suppress T helper cells and inhibit autoimmune demyelination.
    Authors: Mycko Et al.
    J Neurosci 2014;34:8646
  5. CXCR4 and a cell-extrinsic mechanism control immature B lymphocyte egress from bone marrow.
    Authors: Beck Et al.
    J Exp Med 2014;211:2567
  6. Selection of bone metastasis seeds by mesenchymal signals in the primary tumor stroma.
    Authors: Zhang Et al.
    Neoplasia 2013;154:1060
  7. Discovery of very late antigen-4 (VLA-4, alpha4beta1 integrin) allosteric antagonists.
    Authors: Chigaev Et al.
    J Biol Chem 2011;286:5455
  8. Endothelial progenitor cells contribute to the vascularization of endometriotic lesions.
    Authors: Laschke Et al.
    Development 2011;178:442
  9. Noninvasive imaging reveals inhibition of ovarian cancer by targeting CXCL12-CXCR4.
    Authors: Ray Et al.
    Am J Pathol 2011;13:1152

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