Plerixafor (AMD3100)

For research use only. Not for use in humans.

Catalog No.S8030 Synonyms: JM 3100

27 publications

Plerixafor (AMD3100) Chemical Structure

Molecular Weight(MW): 502.78

Plerixafor (AMD3100) 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.

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Selleck's Plerixafor (AMD3100) has been cited by 27 publications

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Biological Activity

Description Plerixafor (AMD3100) 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.
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
CHOK1 cells NX7UO41vTnWwY4Tpc44h[XO|YYm= NWe5TIoxTGm|cHzhZ4Vu\W62IH;mJHsyOjWLXWPESlFidHCqYTDmdo9uKEO[Q2K0JIV5eHKnc4Pl[EBqdiCFSF;LNUBk\WyuczygTWM2OD1yLkixJI5O M{PPdlE4PzF3MUK4
GHOST CXCR4 cell line MV\GeY5kfGmxbjDhd5NigQ>? NVviZmdYUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJI9nKGOxbYDveY5lKGGpYXnud5QhUEmYLUGgUGFKKHO2cnHpckBqdiCJSF;TWEBEYEOUNDDj[YxtKGyrbnWsJGlEPTB;MD65OUBvVQ>? NUnMUY1{OTR4OUixPFk>
HEK293 cells NU\jNo8xTnWwY4Tpc44h[XO|YYm= NHf4SHgzKGSjeYO= MlGzRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgWFIxNXKnc3nzeIFvfCCKSW[xJG5NPC1|IHnu[oVkfGWmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vKGGodHXyJFIh\GG7czygTWM2OD1{LkOgcm0> MV2xPVQ2OTNyNR?=
PBMC cells NGDlWWpHfW6ldHnvckBie3OjeR?= M1HzZ2Vn\mWldHn2[UBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiOEmuOkB{fHKjaX6gbY4hWEKPQzDj[YxteyxiRVO1NF0{Njhibl2= MnOyNVQ3QThzOEm=
human MT4 cells NH7JR4FHfW6ldHnvckBie3OjeR?= M4jyT|Qh\GG7cx?= M1jvWGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gUXQ1KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolzfXNicnXwcIlk[XSrb36gZYZ1\XJiNDDkZZl{KGK7IF3UWEBie3OjeTygSWM2OD12IH7N M3PJZVIxODR|NkO4
human Jurkat cells MmHnSpVv[3Srb36gZZN{[Xl? MVfBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEO[Q2K0JIlvKGi3bXHuJGp2emujdDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOGRkGtbY5lfWOnZDDj[YxtKG2rZ4LheIlwdixiSVO1NF0zPy52IH7N MlPaNVkyQDhyN{G=
MT-4 cells MVLGeY5kfGmxbjDhd5NigQ>? NXvnXoM6TW[oZXP0bZZmKGOxbnPlcpRz[XSrb36gc4Yh[2:vcH;1coQh[WejaX7zeEBJUVZvMTDJTWlDKHO2cnHpckBqdiCPVD20JINmdGy|LDDFR|UxRTZ3IH7N MVyxOFY6QDF6OR?=
rat IR983F cells MoT5SpVv[3Srb36gZZN{[Xl? Mn3kSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZUO[Q1yxNkBnem:vIFPYR3I1KGmwIILheEBKWjl6M1[gZ4VtdHNuIFnDOVA:OTB6IH7N NHPkVHIyQTB3M{e2PC=>
CEM-SS cells M4DjWmZ2dmO2aX;uJIF{e2G7 M1S0fGVn\mWldHn2[UBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiTFHJJJN1emGrbjDpckBETU1vU2OgZ4VtdHNuIFXDOVA:OTJ5IH7N NYf4WGZGOTR4OUixPFk>
human HL60 cells MYfGeY5kfGmxbjDhd5NigQ>? NWrQN2VkTGm|cHzhZ4Vu\W62IH;mJHsyOjWLXWPESlFidHCqYTDmdo9uKEO[Q2K0JIlvKGi3bXHuJGhNPjBiY3XscJMtKEmFNUC9NVUvOiEQvF2= NFHWS|QyQTF6OEC3NS=>
human MOLT4 cells NXThTlJETnWwY4Tpc44h[XO|YYm= NXTsWWczOTByMDDuUS=> NFTQZ3FKdmirYnn0bY9vKG:oIF3hZkAyOkd3IHLpcoRqdmdidH:gR3hEWjRiZYjwdoV{e2WmIHnuJIh2dWGwIF3PUHQ1KGOnbHzzJIF1KDFyMECgcm0h[nliRlHDV{BidmGueYPpdy=> NECySYoyQTR3MUOwOS=>
human MT2 cells MYPGeY5kfGmxbjDhd5NigQ>? MYexJJVoN22O NI\hfmc1KGSjeYO= NUHCZ5R7SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXDJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDwNlQh[W62aXflckBxem:mdXP0bY9vKGG2IEGgeYcwdUxiYX\0[ZIhPCCmYYnzJIJ6KEWOSWPB M4C4VlIyOTZ6M{O2
human U87 cells MoXXSpVv[3Srb36gZZN{[Xl? NY\SZnl2OTByMDDuUS=> NUDtWJFXSW62YXfvcol{fCCjY4Tpeol1gSCjdDDDXGNTPCCrbjDoeY1idiCXOEegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVRF[xMYlv\HWlZXSgcY9lfWyjdHnvckBw\iClQV3QJJBzd2S3Y4Tpc44h[XRiMUCwNEBvVSCkeTDUVk1HWkWWIHHzd4F6 NFrKUW4yPzl3OEO0OC=>

... 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
  • Formulation: PBS
  • Dosages: 5 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 100 mg/mL (198.89 mM)
Water 3 mg/mL warmed (5.96 mM)
DMSO Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 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
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(CN3CCCNCCNCCCNCC3)C=C2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03653247 Recruiting Biological: Plerixafor|Drug: Busulfan|Genetic: BIVV003 Sickle Cell Disease Bioverativ a Sanofi company|Bioverativ Therapeutics Inc. June 28 2019 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
NCT03442673 Recruiting Drug: Vinorelbine|Drug: Gemcitabine|Drug: G-CSF Multiple Myeloma University Hospital Inselspital Berne September 17 2018 Phase 2
NCT03226691 Completed Drug: Plerixafor Sickle Cell Disease National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) July 25 2017 Phase 1

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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.

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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