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Plerixafor (AMD3100) 8HCl CXCR antagonist

Name: Plerixafor (AMD3100) 8HCl
Brand: Selleck Chemicals
SKU: S3013
Availability: InStock
Rating: 5 (50 reviews)

Cat.No.S3013

Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl 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.

Chemical Structure

Molecular Weight: 794.47

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.90%

99.90

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
CHOK1 cells	Function assay			Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50=0.81 nM	17715128
GHOST CXCR4 cell line	Function assay			Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line, IC50=0.95 nM	14698189
HEK293 cells	Function assay		2 days	Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50=2.3 nM	19451305
PBMC cells	Function assay			Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50=3.8 nM	14698189
human MT4 cells	Function assay		4 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay, EC50=4 nM	20043638
human Jurkat cells	Function assay			Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration, IC50=27.4 nM	19188071
MT-4 cells	Function assay			Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50=65 nM	14698189
rat IR983F cells	Function assay			Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50=108 nM	19053768
CEM-SS cells	Function assay			Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50=127 nM	14698189
human HL60 cells	Function assay			Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50=15.2 μM	19188071
human MOLT4 cells	Function assay	1000 nM		Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis	19451305
human MT2 cells	Function assay	1 ug/mL	4 days	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production at 1 ug/mL after 4 days by ELISA	21168336
human U87 cells	Function assay	1000 nM		Antagonist activity at CXCR4 in human U87 cells assessed as inhibition of SDF1-induced modulation of cAMP production at 1000 nM by TR-FRET assay	17958344
MT4	Antiviral assay			Antiviral activity against HIV1 3B assessed as reduction in cytopathic effect in MT4 cells, EC50=0.011μM	17034122
U87	Function assay		15 mins	Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis, IC50=0.695μM	21105715
MT4	Antiviral assay			Antiviral activity against X4-tropic HIV1 NL4.3 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity, EC50=0.062μM	22579418
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days, EC50=0.002μM	22909088
CHO	Function assay			Binding affinity to human recombinant CXCR4 expressed in CHO cells, Kb=0.077μM	22909088
CHO	Function assay			Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis, IC50=0.26μM	22909088
CD44null	Function assay		7 days	Effect on human GBM2 cell differentiation assessed as increase in CD44null cells after 7 days by flow cytometric analysis	22909088
CD44null	Function assay		7 days	Effect on human GBM1 cell differentiation assessed as increase in CD44null cells after 7 days by flow cytometric analysis	22909088
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	794.47	Formula	C₂₈H₅₄N₈.8HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	155148-31-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	JM 3100 8HCl,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride			Smiles	C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl

Solubility

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (37.76mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC₅₀/Ki	CXCL12 ^[1] (Cell-free assay) 5.7 nM CXCR4 ^[1] (Cell-free assay) 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]
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]
References	https://pubmed.ncbi.nlm.nih.gov/19641136/ https://pubmed.ncbi.nlm.nih.gov/16815309/ https://pubmed.ncbi.nlm.nih.gov/22048734/ https://pubmed.ncbi.nlm.nih.gov/22342795/

Applications

Methods	Biomarkers	Images	PMID
Immunofluorescence	CXCR4 β-arrestin2		28521261

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05421416	Not yet recruiting	Stem Cell Transplant Complications	AHS Cancer Control Alberta	April 1 2024	Phase 2
NCT05343572	Recruiting	Asherman Syndrome\|Atrophic Endometrium\|Recurrent Implantation Failure	Hugh Taylor\|Yale University	November 1 2023	Early Phase 1
NCT05844527	Recruiting	Wound of Skin\|Abdominal Wound	MedRegen LLC	November 20 2023	Phase 2
NCT05411575	Withdrawn	COVID-19 Acute Respiratory Distress Syndrome\|COVID-19	4Living Biotech\|4P-Pharma	July 19 2022	Phase 2
NCT05445128	Terminated	Sickle Cell Disease	Ensoma\|bluebird bio	June 24 2022	Phase 2
NCT05835726	Recruiting	Multiple Myeloma\|Daratumumab\|Autologous Stem Cell Transplantation\|Leukapheresis	Fondazione Policlinico Universitario Agostino Gemelli IRCCS	January 1 2022	--

Tech Support

Handling Instructions

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