Plerixafor (AMD3100)

For research use only.

Catalog No.S8030 Synonyms: JM 3100, SID791

72 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.

Selleck's Plerixafor (AMD3100) has been cited by 72 publications

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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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MOLT4 NXHqO2J3TnWwY4Tpc44h[XO|YYm= NF[1UJkyODByIH7N NGTOW21KdmirYnn0bY9vKG:oIF3hZkAyOkd3IHLpcoRqdmdidH:gR3hEWjRiZYjwdoV{e2WmIHnuJIh2dWGwIF3PUHQ1KGOnbHzzJIF1KDFyMECgcm0h[nliRlHDV{BidmGueYPpdy=> M4fqSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NEWxN|A2Lz5zOUS1NVMxPTxxYU6=
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Jurkat MoD0SpVv[3Srb36gZZN{[Xl? NUfqc2pJOC5yMTD0c{AyODBidV2= Mn7BTY5pcWKrdHnvckBw\iCFWFPSOEBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEiLVj3O[YYuVTFvaX7keYNm\CCvaYTvZ4hwdmS{aXHsJI1mdWK{YX7lJIRmeG:uYYLpfoF1cW:wIHH0JFAvODFidH:gNVAxKHWPIHL5JGpEOSCmeXWgZoF{\WRiZnz1c5Jme2OnbnPlJIRmeG:uYYLpfoF1cW:wIHHzd4F6 NYnobYVlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPVE{PjFpPkK2NVkyOzZzPD;hQi=>
MDA-MB-231 NVLVbIFPTnWwY4Tpc44h[XO|YYm= M2PCWVExOCCwTR?= NWf3T3AxOjRiaILz NXLiOJA4SW62YXfvcol{fCCjY4Tpeol1gSCjdDDDXGNTPC2vZXTpZZRm\CClaHXtc5RigGm|IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCFWFPMNVIucW6mdXPl[EBk\WyuIHnueoF{cW:wIHH0JFExOCCwTTDh[pRmeiB{NDDodpMh[nliY4L5d5RidCC4aX;s[ZQhe3SjaX7pcocu[mG|ZXSgcYlkem:|Y3;wbYMhdWG2cnnn[Ywh[XO|YYm= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR7NEi0N{c,Ojl2OUS4OFM9N2F-
TZM-bl NHnY[YJCdnSrdnnyZYwh[XO|YYm= M3r6NFEhcHJ? MoGwRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCKWFKyJJB{\XWmb4\pdpV{KGmwZnXjeIVlKGmwIHj1cYFvKFScTT3icEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKGWwdIL5JJRz\WG2ZXSgNUBpeiCyb4P0JIlv\mWldHnvckBu\WG|dYLl[EBi\nSncjC0PEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6 MnLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{Nk[4OFUoRjJ6Mk[2PFQ2RC:jPh?=
CXCR4+ NFvaUnFHfW6ldHnvckBie3OjeR?= NGrPXYU3KG2pL3vn NHPROY4zKGi{cx?= NGXESmxKdmS3Y4Tpc44hcGWvYYTvdI9q\XSrYzDzeIVuKGOnbHygcY9jcWyrenH0bY9vKGmwIFO1O2JNNzZibX;1d4Uh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gR3hEWjRtIHPlcIx{KGmwIHLsc49lKGG2IE[gcYcwc2duIIPjJI1m[XO3cnXkJIFnfGW{IEKgbJJ{KGK7IFHQR{1kd26sdXfheIVlKGGwdHmtR3hEWjRvc4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2comgdoVt[XSrdnWgeI8hfmWqaXPs[UBkd262cn;s MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTNzNEi0NEc,Ojl|MUS4OFA9N2F-

... 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

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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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:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04646603 Active not recruiting Drug: MRG-001|Drug: Placebo COVID-19 MedRegen LLC|ICON plc January 28 2021 Phase 1|Phase 2
NCT03547830 Recruiting Drug: Plerixafor|Drug: Gcsf Chronic Granulomatous Disease Federal Research Institute of Pediatric Hematology Oncology and Immunology April 13 2019 Phase 2
NCT03653247 Recruiting Biological: Plerixafor|Drug: Busulfan|Genetic: BIVV003 Sickle Cell Disease Bioverativ a Sanofi company|Sanofi March 6 2019 Phase 1|Phase 2
NCT03442673 Recruiting Drug: Vinorelbine|Drug: Gemcitabine|Drug: G-CSF Multiple Myeloma University Hospital Inselspital Berne September 17 2018 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