AMD 3100 octahydrochloride

Cat. No. 3299

AMD 3100 octahydrochloride C28H54N8.8HCl [155148-31-5]

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Alternative 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

Soluble to 100 mM in water
Desiccate at -20°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Paganessi et al (2011) Effective mobilization of hematopoietic progenitor cells in G-CSF mobilization defective CD26-/- mice through AMD3100-induced disruption of the CXCL12-CXCR4 axis. Exp.Hematol. 39 384. PMID: 21168468.

Hogaboam et al (2005) The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease. Pharmacol.Ther. 107 314. PMID: 16009428.

Hatse et al (2002) Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4. FEBS Letts. 527 255.

Bridger et al (1995) 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. J.Med.Chem. 38 366. PMID: 7830280.

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Citations are publications that use Tocris products. Selected citations for AMD 3100 octahydrochloride include:

Cavnar et al (2015) Modeling selective elimination of quiescent cancer cells from bone marrow. Cell 17 625. PMID: 26408255.

Chu et al (2015) CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. Neoplasia 10 e0133616. PMID: 26214690.

Beck et al (2014) CXCR4 and a cell-extrinsic mechanism control immature B lymphocyte egress from bone marrow. J Exp Med 211 2567. PMID: 25403444.

Farkas et al (2014) CXCR4 inhibition ameliorates severe obliterative pulmonary hypertension and accumulation of C-kit+ cells in rats. PLoS One 9 e89810. PMID: 24587052.

Mycko et al (2014) Brain glycolipids suppress T helper cells and inhibit autoimmune demyelination. J Neurosci 34 8646. PMID: 24948818.

Zhang et al (2013) Selection of bone metastasis seeds by mesenchymal signals in the primary tumor stroma. Neoplasia 154 1060. PMID: 23993096.

Chigaev et al (2011) Discovery of very late antigen-4 (VLA-4, alpha4beta1 integrin) allosteric antagonists. J Biol Chem 286 5455. PMID: 21131351.

Laschke et al (2011) Endothelial progenitor cells contribute to the vascularization of endometriotic lesions. Development 178 442. PMID: 21224081.

Ray et al (2011) Noninvasive imaging reveals inhibition of ovarian cancer by targeting CXCL12-CXCR4. Am J Pathol 13 1152. PMID: 22241961.

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Keywords: AMD 3100 octahydrochloride, supplier, selective, CXCR4, antagonists, Chemokine, Receptors, AMD3100, octahydrochloride, JM3100, Tocris Bioscience, Chemokine CXC Receptor Antagonist products

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