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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3 Customer Reviews

  • 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.

    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.

  • 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.

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Choose Selective CXCR Inhibitors

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 Moi5SpVv[3Srb36gZZN{[Xl? MlTTSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZVOGRkHhcJBp[SCocn;tJGNZS1J2IHX4dJJme3OnZDDpckBEUE:NMTDj[YxteyxiSVO1NF0xNjhzIH7N NWHxdFRoOTd5MUWxNlg>
GHOST CXCR4 cell line NFnDUVhHfW6ldHnvckBie3OjeR?= NF7a[YdKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gc4Yh[2:vcH;1coQh[WejaX7zeEBJUVZvMTDMRWkhe3S{YXnuJIlvKEeKT2PUJGNZS1J2IHPlcIwhdGmwZTygTWM2OD1yLkm1JI5O NX35NnZKOTR4OUixPFk>
HEK293 cells MnzDSpVv[3Srb36gZZN{[Xl? NX\6XplyOiCmYYnz M2jpVGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JHQzOC2{ZYPpd5RidnRiSFnWNUBPVDRvMzDpcoZm[3SnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYLhcEBz\XCuaXPheIlwdiCjZoTldkAzKGSjeYOsJGlEPTB;Mj6zJI5O Ml;WNVk1PTF|MEW=
PBMC cells NYSwbmdiTnWwY4Tpc44h[XO|YYm= MVHF[oZm[3SrdnWgZ49v[2WwdILheIlwdiCxZjDjc41xd3WwZDDh[4FqdnO2IFjJWk0yKDh7Lk[gd5Rz[WmwIHnuJHBDVUNiY3XscJMtKEWFNUC9N{45KG6P MXqxOFY6QDF6OR?=
human MT4 cells MVLGeY5kfGmxbjDhd5NigQ>? NHHEcno1KGSjeYO= NXK1dXd6SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXK3czDy[ZBtcWOjdHnvckBi\nSncjC0JIRigXNiYomgUXRVKGG|c3H5MEBGSzVyPUSgcm0> MXeyNFA1OzZ|OB?=
human Jurkat cells NGG0OmZHfW6ldHnvckBie3OjeR?= MV3BcpRi\2:waYP0JIFkfGm4aYT5JIF1KEO[Q2K0JIlvKGi3bXHuJGp2emujdDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOGRkGtbY5lfWOnZDDj[YxtKG2rZ4LheIlwdixiSVO1NF0zPy52IH7N MWmxPVE5QDB5MR?=
MT-4 cells M1TmOWZ2dmO2aX;uJIF{e2G7 NI\FSphG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBi\2GrboP0JGhKXi1zIFnJTWIhe3S{YXnuJIlvKE2WLUSgZ4VtdHNuIFXDOVA:PjVibl2= NHe3cmYyPDZ7OEG4PS=>
rat IR983F cells MV7GeY5kfGmxbjDhd5NigQ>? NUP0U5NNTGm|cHzhZ4Vu\W62IH;mJHsyOjWLXVPYR2wyOiCocn;tJGNZS1J2IHnuJJJifCCLUkm4N2Yh[2WubIOsJGlEPTB;MUC4JI5O Mo\mNVkxPTN5Nki=
CEM-SS cells NHHzXW1HfW6ldHnvckBie3OjeR?= MXjF[oZm[3SrdnWgZ49v[2WwdILheIlwdiCxZjDjc41xd3WwZDDh[4FqdnO2IFjJWk0yKEyDSTDzeJJicW5iaX6gR2VONVOVIHPlcIx{NCCHQ{WwQVEzPyCwTR?= M1PMSlE1Pjl6MUi5
human HL60 cells M4XpdmZ2dmO2aX;uJIF{e2G7 M{XhPWRqe3CuYXPlcYVvfCCxZjDbNVI2UV2VRF[xZYxxcGFiZoLvcUBEYEOUNDDpckBpfW2jbjDIUFYxKGOnbHzzMEBKSzVyPUG1MlIh|ryP M{PvTlE6OTh6MEex
human MOLT4 cells MUPGeY5kfGmxbjDhd5NigQ>? MWSxNFAxKG6P M3XuT2lvcGmkaYTpc44hd2ZiTXHiJFEzTzViYnnu[Ilv\yC2bzDDXGNTPCCneIDy[ZN{\WRiaX6gbJVu[W5iTV;MWFQh[2WubIOgZZQhOTByMDDuUUBjgSCIQVPTJIFv[Wy7c3nz M3H1[|E6PDVzM{C1
human MT2 cells MmLnSpVv[3Srb36gZZN{[Xl? NFe5WWoyKHWpL33M NITqWlY1KGSjeYO= NVLwWnVvSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXDJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDwNlQh[W62aXflckBxem:mdXP0bY9vKGG2IEGgeYcwdUxiYX\0[ZIhPCCmYYnzJIJ6KEWOSWPB NHLxSIwzOTF4OEOzOi=>
human U87 cells MX7GeY5kfGmxbjDhd5NigQ>? NWW2dVdiOTByMDDuUS=> NGG3doRCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFPYR3I1KGmwIHj1cYFvKFV6NzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOGRkGtbY5lfWOnZDDtc4R2dGG2aX;uJI9nKGODTWCgdJJw\HWldHnvckBifCBzMECwJI5OKGK7IGTSMWZTTVRiYYPzZZk> MU[xO|k2QDN2NB?=

... 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:
30% propylene glycol, 5% Tween 80, 65% D5W
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
Synonyms JM 3100

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01026987 Completed Stem Cell Transplant Patients Washington University School of Medicine April 29, 2010 Phase 1
NCT02231879 Recruiting Myelokathexis|WHIMS|Neutropenia|Warts National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 27, 2014 Phase 3
NCT01547806 Active, not recruiting Plasma Cell Myeloma|Multiple Myeloma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 22, 2012 Phase 2
NCT01331018 Recruiting Fanconi Anemia Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI)|National Heart, Lung, and Blood Institute (NHLBI) February 22, 2012 Phase 1
NCT02989701 Recruiting Sickle Cell Disease Without Crisis Alessandra Biffi|Boston Children’s Hospital January 2017 Phase 1
NCT02790957 Recruiting Diabetes|Wounds|Critical Limb Ischemia Gian Paolo Fadini|University Hospital Padova|University of Padova June 2016 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.

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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