Plerixafor (AMD3100)

Catalog No.S8030 Synonyms: JM 3100

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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Cited by 14 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 (AMD3100) 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 (AMD3100) purchased from Selleck.

  • a, ECs were seeded onto collagen gels containing CXCL12 and incubated with vehicle (DMSO) control or AMD3100 (1 μM), rapamycin (100 nM), or PP242 (600 nM) for 24 h after before fixing and imaging. Scale bar = 150 μm. b, The average number of invading cells was calculated by counting five wells per condition.

    Angiogenesis, 2016, 19(3):359-71. Plerixafor (AMD3100) purchased from Selleck.

  • (A) Pictures display representative results of the change of invading cells after incubation of human FTC cell line TT2609-C02 with different concentrations of CXCR4 antagonists AMD3100 and WZ811 as well as rh-SDF1α as receptor agonist. Cells were visualized by DAPI staining. (B) Invading cells were counted in five visual fields of at least three different membranes. Differences after treatment are illustrated as fold change to control.

    J Cancer, 2018, 9(6):929-940. Plerixafor (AMD3100) purchased from Selleck.

Purity & Quality Control

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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 M{PueWZ2dmO2aX;uJIF{e2G7 M2POSmRqe3CuYXPlcYVvfCCxZjDbNVI2UV2VRF[xZYxxcGFiZoLvcUBEYEOUNDDlfJBz\XO|ZXSgbY4hS0iRS{GgZ4VtdHNuIFnDOVA:OC56MTDuUS=> M{\y[|E4PzF3MUK4
GHOST CXCR4 cell line NV7KZ3U5TnWwY4Tpc44h[XO|YYm= NF3FTIlKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gc4Yh[2:vcH;1coQh[WejaX7zeEBJUVZvMTDMRWkhe3S{YXnuJIlvKEeKT2PUJGNZS1J2IHPlcIwhdGmwZTygTWM2OD1yLkm1JI5O NIfaeJMyPDZ7OEG4PS=>
HEK293 cells NX3kb5gxTnWwY4Tpc44h[XO|YYm= NGXaZXQzKGSjeYO= MmDCRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgWFIxNXKnc3nzeIFvfCCKSW[xJG5NPC1|IHnu[oVkfGWmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vKGGodHXyJFIh\GG7czygTWM2OD1{LkOgcm0> NH3BUYoyQTR3MUOwOS=>
PBMC cells NVHQfZB3TnWwY4Tpc44h[XO|YYm= M1\zNWVn\mWldHn2[UBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiOEmuOkB{fHKjaX6gbY4hWEKPQzDj[YxteyxiRVO1NF0{Njhibl2= MoLTNVQ3QThzOEm=
human MT4 cells MXPGeY5kfGmxbjDhd5NigQ>? MX20JIRigXN? MmjVRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSB|QjDpcoZm[3SnZDDpckBpfW2jbjDNWFQh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJ2eyC{ZYDsbYNifGmxbjDh[pRmeiB2IHThfZMh[nliTWTUJIF{e2G7LDDFR|UxRTRibl2= M4jt[VIxODR|NkO4
human Jurkat cells NH7WVZRHfW6ldHnvckBie3OjeR?= NEnhNI9CdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFPYR3I1KGmwIHj1cYFvKEq3cnvheEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPESlEucW6mdXPl[EBk\WyuIH3p[5JifGmxbjygTWM2OD1{Nz60JI5O NEmzSpcyQTF6OEC3NS=>
MT-4 cells MVXGeY5kfGmxbjDhd5NigQ>? M4fpT2Vn\mWldHn2[UBkd26lZX70doF1cW:wIH;mJINwdXCxdX7kJIFo[Wmwc4SgTGlXNTFiSVnJRkB{fHKjaX6gbY4hVVRvNDDj[YxteyxiRVO1NF03PSCwTR?= MYWxOFY6QDF6OR?=
rat IR983F cells MUHGeY5kfGmxbjDhd5NigQ>? MX7EbZNxdGGlZX3lcpQhd2ZiW{GyOWleS1iFTEGyJIZzd21iQ2jDVlQhcW5icnH0JGlTQTh|RjDj[YxteyxiSVO1NF0yODhibl2= M4rtVVE6ODV|N{[4
CEM-SS cells Mk\rSpVv[3Srb36gZZN{[Xl? NHfud4pG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBi\2GrboP0JGhKXi1zIFzBTUB{fHKjaX6gbY4hS0WPLWPTJINmdGy|LDDFR|UxRTF{NzDuUS=> M2i5fFE1Pjl6MUi5
human HL60 cells NHHUe2pHfW6ldHnvckBie3OjeR?= M{PRUWRqe3CuYXPlcYVvfCCxZjDbNVI2UV2VRF[xZYxxcGFiZoLvcUBEYEOUNDDpckBpfW2jbjDIUFYxKGOnbHzzMEBKSzVyPUG1MlIh|ryP Mo[wNVkyQDhyN{G=
human MOLT4 cells NIHQRmtHfW6ldHnvckBie3OjeR?= NWPFSpR3OTByMDDuUS=> NHvr[GxKdmirYnn0bY9vKG:oIF3hZkAyOkd3IHLpcoRqdmdidH:gR3hEWjRiZYjwdoV{e2WmIHnuJIh2dWGwIF3PUHQ1KGOnbHzzJIF1KDFyMECgcm0h[nliRlHDV{BidmGueYPpdy=> M4DvfFE6PDVzM{C1
human MT2 cells Ml3MSpVv[3Srb36gZZN{[Xl? MV6xJJVoN22O NWe4[3lNPCCmYYnz MmPJRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSB|QjDpcoZm[3SnZDDpckBpfW2jbjDNWFIh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCCyMkSgZY51cWenbjDwdo9lfWO2aX;uJIF1KDFidXevcWwh[W[2ZYKgOEBl[Xm|IHL5JGVNUVOD M2HaN|IyOTZ6M{O2
human U87 cells MWjGeY5kfGmxbjDhd5NigQ>? NXrC[oJGOTByMDDuUS=> M3Ww[2FvfGGpb37pd5Qh[WO2aY\peJkh[XRiQ2jDVlQhcW5iaIXtZY4hXTh5IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhW0SIMT3pcoR2[2WmIH3v[JVt[XSrb36gc4Yh[0GPUDDwdo9lfWO2aX;uJIF1KDFyMECgcm0h[nliVGKtSnJGXCCjc4PhfS=> M2nTWFE4QTV6M{S0

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03653247 Recruiting Sickle Cell Disease Bioverativ - a sanofi company|Bioverativ Therapeutics Inc. December 14 2018 Phase 1|Phase 2
NCT03746080 Recruiting Glioblastoma|Glioblastoma With Primitive Neuronal Component|Gliosarcoma|Malignant Glioma|Oligodendroglial Component Present Lawrence Recht|Sanofi|Stanford University December 4 2018 Phase 2
NCT03746080 Recruiting Glioblastoma|Glioblastoma With Primitive Neuronal Component|Gliosarcoma|Malignant Glioma|Oligodendroglial Component Present Lawrence Recht|Sanofi|Stanford University December 4 2018 Phase 2
NCT03653247 Recruiting Sickle Cell Disease Bioverativ - a sanofi company|Bioverativ Therapeutics Inc. December 14 2018 Phase 1|Phase 2
NCT03664830 Recruiting Sickle Cell Disease City of Hope Medical Center September 19 2018 Phase 1
NCT03664830 Recruiting Sickle Cell Disease City of Hope Medical Center September 19 2018 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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Tel: +1-832-582-8158 Ext:3

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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