Plerixafor 8HCl (AMD3100 8HCl)

For research use only.

Catalog No.S3013 Synonyms: JM 3100 8HCl

11 publications

Plerixafor 8HCl (AMD3100 8HCl) Chemical Structure

CAS No. 155148-31-5

Plerixafor 8HCl (AMD3100, JM 3100) is the hydrochloride of Plerixafor, 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 can be used as an anti-HIV agent.

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Selleck's Plerixafor 8HCl (AMD3100 8HCl) has been cited by 11 publications

4 Customer Reviews

  • BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.

    Blood 2014 123(21), 3296-304. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

    Chemotaxis (Transwell invasion) assay showing the migration of BMSCs in response to CXCL12 (0–100 ng/ml) and the inhibitory effect of the CXCR4 antagonist AMD3100 (5 mg/ml, 30 min). *P < 0.05, compared with the control group (no treatment); #P < 0.05; n = 4 wells from separate cultures.

    J Clin Invest, 2015, 125(8): 3226-40. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

  • Inhibition of SDF-1α signalling in subchondral bone attenuated cartilage degeneration (A) H&E staining of tibia subchondral bone and cartilage from sham, ACLT/PBS, and ACLT/AMD3100 groups. Calibration scale: bar = 100 μm; (B) Safranin O-Fast Green staining of articular cartilage in sagittal sections of tibia from mice treated with PBS or AMD3100 and sacrificed 30 days post ACLT or sham surgery. Calibration scale: bar = 100 μm; (C) MMP13 expression was detected by immunohistochemical staining of cartilage, and representative images are shown. A positive signal was indicated by the brown colour and marked by black arrows, meanwhile a negative control was present. Calibration scale: bar = 50 μm; (D) OARSI scores of sham or ACLT mice treated with PBS or AMD3100.Quantitative analysis of the percentage of MMP13+ chondrocytes in articular cartilage tissue sections in each group, reported as means ± SD. n = 10. * ACLT/PBS different from sham/PBS (p < 0.05), # ACLT/PBS different from ACLT/AMD3100 (p < 0.05).

    Int J Mol Sci, 2016, 17(6): 943.. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

    CXCR4 is overexpressed in primary osteosarcoma cells and promotes invasion in U2OS cells. (A) We obtained primary cells derived from three patients suffering from osteosarcoma. The splitting of tumor tissues were performed by western blot analysis. The expression of CXCR4 in primary osteosarcoma cells were detected. OS1, OS2, OS3, three primary osteosarcoma cells. (B) Suppression of CXCR4 by plerixafor (CXCR4 inhibitor, 500 ng/ml, 48 h) downregulates the expression of MMP-2 and MMP-9. The downregulation can be reversed by SDF-1 (100 ng/ml, pre-incubate for 2 h). Sinomenine treatment had similar effect to plerixafor. The bands were quantitative analyzed by ImageJ software. *P<0.05, versus control. NS, no significance. #P<0.05 compare with plerixafor treatment. (C) Cells were treated with plerixafor and sinomenine, with or without SDF-1 simultaneously for 24 h. Then cells were harvested for Transwell assay. Representative images are presented. (x200 magnification).

    Int J Oncol, 2016, 48(5):2098-112.. Plerixafor 8HCl (AMD3100 8HCl) purchased from Selleck.

Purity & Quality Control

Choose Selective CXCR Inhibitors

Biological Activity

Description Plerixafor 8HCl (AMD3100, JM 3100) is the hydrochloride of Plerixafor, 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 can be used as an anti-HIV agent.
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 MoX2SpVv[3Srb36gZZN{[Xl? MnntSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZVOGRkHhcJBp[SCocn;tJGNZS1J2IHX4dJJme3OnZDDpckBEUE:NMTDj[YxteyxiSVO1NF0xNjhzIH7N NU\KOmRROTd5MUWxNlg>
GHOST CXCR4 cell line MWDGeY5kfGmxbjDhd5NigQ>? MW\Jcohq[mm2b4L5JINwdmOnboTyZZRqd25ib3[gZ49ueG:3bnSgZYdicW6|dDDITXYuOSCOQVmgd5Rz[WmwIHnuJGdJV1OWIFPYR3I1KGOnbHygcIlv\SxiSVO1NF0xNjl3IH7N M4qxOVE1Pjl6MUi5
HEK293 cells MWjGeY5kfGmxbjDhd5NigQ>? NVnDbo05OiCmYYnz NE[5WIJCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBVOjBvcnXzbZN1[W62IFjJWlEhVkx2LUOgbY5n\WO2ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25iYX\0[ZIhOiCmYYnzMEBKSzVyPUKuN{BvVQ>? MmHuNVk1PTF|MEW=
PBMC cells NUj6SHRJTnWwY4Tpc44h[XO|YYm= NIOxVZZG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBi\2GrboP0JGhKXi1zIEi5MlYhe3S{YXnuJIlvKFCETVOgZ4VtdHNuIFXDOVA:Oy56IH7N MlvGNVQ3QThzOEm=
human MT4 cells MljqSpVv[3Srb36gZZN{[Xl? MlHmOEBl[Xm| NYPve|FoSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXK3czDy[ZBtcWOjdHnvckBi\nSncjC0JIRigXNiYomgUXRVKGG|c3H5MEBGSzVyPUSgcm0> MnjWNlAxPDN4M{i=
human Jurkat cells NXrrW5B{TnWwY4Tpc44h[XO|YYm= MY\BcpRi\2:waYP0JIFkfGm4aYT5JIF1KEO[Q2K0JIlvKGi3bXHuJGp2emujdDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOGRkGtbY5lfWOnZDDj[YxtKG2rZ4LheIlwdixiSVO1NF0zPy52IH7N NGL6eYwyQTF6OEC3NS=>
MT-4 cells M{jqTmZ2dmO2aX;uJIF{e2G7 NH3uUVlG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBi\2GrboP0JGhKXi1zIFnJTWIhe3S{YXnuJIlvKE2WLUSgZ4VtdHNuIFXDOVA:PjVibl2= M4DYOFE1Pjl6MUi5
rat IR983F cells MXvGeY5kfGmxbjDhd5NigQ>? Ml3tSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZUO[Q1yxNkBnem:vIFPYR3I1KGmwIILheEBKWjl6M1[gZ4VtdHNuIFnDOVA:OTB6IH7N M3f3cFE6ODV|N{[4
CEM-SS cells MnHsSpVv[3Srb36gZZN{[Xl? NUTGWmlrTW[oZXP0bZZmKGOxbnPlcpRz[XSrb36gc4Yh[2:vcH;1coQh[WejaX7zeEBJUVZvMTDMRWkhe3S{YXnuJIlvKEOHTT3TV{Bk\WyuczygSWM2OD1zMkegcm0> MYCxOFY6QDF6OR?=
human HL60 cells MkH1SpVv[3Srb36gZZN{[Xl? MWTEbZNxdGGlZX3lcpQhd2ZiW{GyOWleW0SIMXHsdIhiKG[{b32gR3hEWjRiaX6gbJVu[W5iSFy2NEBk\WyuczygTWM2OD1zNT6yJO69VQ>? NGPYPHUyQTF6OEC3NS=>
human MOLT4 cells MWjGeY5kfGmxbjDhd5NigQ>? MXexNFAxKG6P M{fINGlvcGmkaYTpc44hd2ZiTXHiJFEzTzViYnnu[Ilv\yC2bzDDXGNTPCCneIDy[ZN{\WRiaX6gbJVu[W5iTV;MWFQh[2WubIOgZZQhOTByMDDuUUBjgSCIQVPTJIFv[Wy7c3nz NUfHcoFCOTl2NUGzNFU>
human MT2 cells NXfOXFF7TnWwY4Tpc44h[XO|YYm= M3\mXlEhfWdxbVy= Ml3mOEBl[Xm| NHnRdI9CdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIEPCJIlv\mWldHXkJIlvKGi3bXHuJG1VOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqemGuIICyOEBidnSrZ3XuJJBzd2S3Y4Tpc44h[XRiMTD1[{9uVCCjZoTldkA1KGSjeYOgZpkhTUyLU1G= MXiyNVE3QDN|Nh?=
human U87 cells NHPUPZlHfW6ldHnvckBie3OjeR?= NIrVUIoyODByIH7N NFj4UHJCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFPYR3I1KGmwIHj1cYFvKFV6NzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOGRkGtbY5lfWOnZDDtc4R2dGG2aX;uJI9nKGODTWCgdJJw\HWldHnvckBifCBzMECwJI5OKGK7IGTSMWZTTVRiYYPzZZk> NFrPSoYyPzl3OEO0OC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID

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.


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]


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 100 mg/mL (125.87 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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 794.47


CAS No. 155148-31-5
Storage powder
in solvent
Synonyms JM 3100 8HCl

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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|Sanofi 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
NCT02989701 Completed Drug: Plerixafor Sickle Cell Disease Without Crisis Alessandra Biffi|Boston Children''s Hospital January 2017 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID