AMD 3100 octahydrochloride
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Description: Highly selective CXCR4 antagonist
Alternative Names: JM 3100, Plerixafor
Chemical Name: 1,1'-[1,4-Phenylenebis-(methylene)]-bis-(1,4,8,11-tetraazacyclotetradecane) octahydrochloride
Biological Activity
AMD 3100 octahydrochloride is a highly selective CXCR4 chemokine receptor antagonist (IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and most other chemokine receptors, respectively). Also CXCR7 allosteric agonist. 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. Attenuates cocaine place preference and locomotor stimulation in rats. Attenuates microglial activation neurological function after ischemic stroke in mice. Inhibits tumor cell migration and proliferation in vitro and in vivo in a range of cancers.Technical Data
M.Wt:
794.48
Formula:
C28H54N8.8HCl
Solubility:
Soluble to 100 mM in water
Storage:
Store at -20°C
CAS No:
155148-31-5
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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 -
The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease.
Hogaboam et al.
Pharmacol.Ther., 2005;107:314 -
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 -
Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4.
Hatse et al.
FEBS Letts., 2002;527:255 -
Chemokines and cocaine: CXCR4 receptor antagonist AMD3100 attenuates cocaine place preference and locomotor stimulation in rats.
Kim et al.
Brain Behav.Immun., 2017;62:30 -
A novel CXCR4 antagonist CX549 induces neuroprotection in stroke brain.
Wu et al.
Cell.Transplant., 2017;26:571 -
CXCR4 antagonists: targeting the microenvironment in leukemia and other cancers.
Burger and Peled et al.
Leukemia, 2009;23:43 -
MD3100 Is a CXCR7 ligand with allosteric agonist properties.
Kalatskaya et al.
Mol.Pharmacol,, 2009;75:1240
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Citations for AMD 3100 octahydrochloride
The citations listed below are publications that use Tocris products. Selected citations for AMD 3100 octahydrochloride include:
16 Citations: Showing 1 - 10
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Oral Pathobiont Activates Anti-Apoptotic Pathway, Promoting both Immune Suppression and Oncogenic Cell Proliferation.
Authors: Arjunan Et al.
Sci Rep 2018;8:16607
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Anti-fibrotic effects of CXCR4-targeting i-body AD-114 in preclinical models of pulmonary fibrosis.
Authors: Griffiths
Sci Rep 2018;8(1):3212
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Circadian Expression of Migratory Factors Establishes Lineage-Specific Signatures that Guide the Homing of Leukocyte Subsets to Tissues.
Authors: He Et al.
Immunity 2018;49:1175
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CXCR4-expressing Mist1 + progenitors in the gastric antrum contribute to gastric cancer development.
Authors: Sakitani
Oncotarget 2017;8(67):111012
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Agarose Spot as a Comparative Method for in situ Analysis of Simultaneous Chemotactic Responses to Multiple Chemokines.
Authors: Ahmed Et al.
Sci Rep 2017;7:1075
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Modeling selective elimination of quiescent cancer cells from bone marrow.
Authors: Cavnar Et al.
Cell 2015;17:625
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CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis.
Authors: Chu Et al.
Neoplasia 2015;10:e0133616
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Macrophage Migration Inhibitory Factor Mediates PAR-Induced Bladder Pain.
Authors: Kouzoukas Et al.
PLoS One 2015;10:e0127628
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CXCR4 inhibition ameliorates severe obliterative pulmonary hypertension and accumulation of C-kit+ cells in rats.
Authors: Farkas Et al.
PLoS One 2014;9:e89810
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Brain glycolipids suppress T helper cells and inhibit autoimmune demyelination.
Authors: Mycko Et al.
J Neurosci 2014;34:8646
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CXCR4 and a cell-extrinsic mechanism control immature B lymphocyte egress from bone marrow.
Authors: Beck Et al.
J Exp Med 2014;211:2567
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Selection of bone metastasis seeds by mesenchymal signals in the primary tumor stroma.
Authors: Zhang Et al.
Neoplasia 2013;154:1060
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Rhythmic modulation of the hematopoietic niche through neutrophil clearance.
Authors: Casanova-Acebes Et al.
Cell 2013;153:1025
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Discovery of very late antigen-4 (VLA-4, alpha4beta1 integrin) allosteric antagonists.
Authors: Chigaev Et al.
J Biol Chem 2011;286:5455
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Endothelial progenitor cells contribute to the vascularization of endometriotic lesions.
Authors: Laschke Et al.
Development 2011;178:442
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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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