Plerixafor (AMD3100)

For research use only.

Catalog No.S8030 Synonyms: JM 3100, SID791

67 publications

Plerixafor (AMD3100) Chemical Structure

CAS No. 110078-46-1

Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

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Selleck's Plerixafor (AMD3100) has been cited by 67 publications

Purity & Quality Control

Choose Selective CXCR Inhibitors

Biological Activity

Description Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.
Targets
CXCL12 [1]
(Cell-free assay)
CXCR4 [1]
(Cell-free assay)
5.7 nM 44 nM
In vitro

Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. [1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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TZM-bl NUHmXlJVSW62aY\pdoFtKGG|c3H5 M4O0XVEhcHJ? MkLvRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCKWFKyJJB{\XWmb4\pdpV{KGmwZnXjeIVlKGmwIHj1cYFvKFScTT3icEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKGWwdIL5JJRz\WG2ZXSgNUBpeiCyb4P0JIlv\mWldHnvckBu\WG|dYLl[EBi\nSncjC0PEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6 Ml72QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{Nk[4OFUoRjJ6Mk[2PFQ2RC:jPh?=
CXCR4+ M2rINGZ2dmO2aX;uJIF{e2G7 MWm2JI1oN2up M1TKb|IhcHK| MnjzTY5lfWO2aX;uJIhmdWG2b4DvbYV1cWNic4TlcUBk\WyuIH3vZoltcXqjdHnvckBqdiCFNUfCUE83KG2xdYPlJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIFPYR3I1MyClZXzsd{BqdiCkbH;v[EBifCB4IH3nM4toNCC|YzDt[YF{fXKnZDDh[pRmeiB{IHjyd{BjgSCDUFOtZ49vcnWpYYTl[EBidnSrLVPYR3I1NXO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7IILlcIF1cX[nIITvJJZmcGmlbHWgZ49vfHKxbB?= NHn5S4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOxOFg1OCd-MkmzNVQ5PDB:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Immunofluorescence
CXCR4; 

PubMed: 28521261     


Representative immunofluorescence images of competition-binding affinity assay of three selected compounds compared to AMD3100. CXCR4 receptors on the cell surface are shown in red fluorescent color in this binding affinity assay using biotinylated TN14003 that binds to CXCR4. When our test compounds are preincubated with the cells and block the binding of biotinylated TN14003, the red fluorescent color gets reduced. The effective concentration (EC) of AMD3100 was 1000 nM, while compounds Ie, IIj and Iq showed much better EC of only 1, 1 and 10 nM, respectively.

β-arrestin2; 

PubMed: 31186083     


Confocal microscopy analysis of CXCR4 and BA2 in Jurkat cells pretreated with vehicle, AMD3100, or X4-2-6 and stimulated with CXCL12, as indicated. Arrows indicate CXCR4 (red), BA2 (green), or colocalization (orange). Images are representative of three independent experiments. Scale bars, 10 μM. DAPI, 4′,6-diamidino-2-phenylindole, dihydrochloride.

28521261 31186083
In vivo A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. [3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. [4]

Protocol

Animal Research:[4]
- Collapse
  • Animal Models: Twelve-week-old C57BL/6 mice with segmental bone defect
  • Dosages: 5 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 3 mg/mL warmed (5.96 mM)
DMSO Insoluble
Ethanol ''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 502.78
Formula

C28H54N8

CAS No. 110078-46-1
Storage powder
in solvent
Synonyms JM 3100, SID791
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03547830 Recruiting Drug: Plerixafor|Drug: Gcsf Chronic Granulomatous Disease Federal Research Institute of Pediatric Hematology Oncology and Immunology April 13 2019 Phase 2
NCT02989701 Completed Drug: Plerixafor Sickle Cell Disease Without Crisis Alessandra Biffi|Boston Children''s Hospital January 2017 Phase 1
NCT03406091 Active not recruiting Drug: Plerixafor Multiple Myeloma Fondazione EMN Italy Onlus November 26 2015 --
NCT02200380 Terminated Drug: CDX-301|Drug: CDX-301 and plerixafor For Donors|Related Donors Giving Peripheral Blood Stem Cells (PBSC) to a Sibling|For Recipients|Acute Myelogenous Leukemia (AML)|Acute Lymphoblastic Leukemia (ALL)|Myelodysplastic Syndrome (MDS)|Chronic Myelogenous Leukemia (CML)|Non-Hodgkins Lymphoma (NHL)|Hodgkins Disease (HD)|Chronic Lymphocytic Leukemia (CLL) Celldex Therapeutics July 2014 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    How about the half-life of the product (Cat S8030)?

  • Answer:

    The biological half-life for this drug is 3-5 hours: https://en.wikipedia.org/wiki/Plerixafor.

CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID