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Plerixafor (AMD3100) 8HCl CXCR Antagoniste

Name: Plerixafor (AMD3100) 8HCl
Brand: Selleck Chemicals
SKU: S3013
Rating: 5 (53 reviews)

Réf. Catalogue: S3013

Plerixafor (AMD3100, JM 3100, Plerixafor Octahydrochlorure, AMD3100 octahydrochlorure, SID791 octahydrochlorure) 8HCl est le chlorhydrate de Plerixafor, un antagoniste du récepteur des chimiokines pour CXCR4 et la chimiotaxie médiatisée par CXCL12 avec des IC50 de 44 nM et 5,7 nM dans des essais sans cellules, respectivement. Plerixafor peut être utilisé comme agent anti-HIV.

Plerixafor (AMD3100) 8HCl CXCR Antagoniste Chemical Structure

Structure chimique

Poids moléculaire: 794.47

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.90%

99.90

Cibles apparentées	Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
Autre CXCR Inhibiteurs	AZD5069 SB 225002 Reparixin (Repertaxin) WZ811 Navarixin (SCH-527123) LIT-927 SX-682 AMG 487 SB 265610 LY2510924

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Description de l'activité	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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	794.47	Formule	C₂₈H₅₄N₈.8HCl	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	155148-31-5	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	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

Solubilité (Solubility)

In vitro
Lot:

Water : 100 mg/mL

DMSO : Insoluble
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Clear solution	Saline Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Targets/IC₅₀/Ki	CXCL12 (Cell-free assay) 5.7 nM CXCR4 (Cell-free assay) 44 nM
In vitro	Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. 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.
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. 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.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/19641136/ [2] https://pubmed.ncbi.nlm.nih.gov/16815309/ [3] https://pubmed.ncbi.nlm.nih.gov/22048734/ [4] https://pubmed.ncbi.nlm.nih.gov/22342795/

Applications (Applications)

Méthodes	Biomarqueurs	Images	PMID
Immunofluorescence	CXCR4 β-arrestin2		28521261

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2026-09-03)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT06851767	ENROLLING_BY_INVITATION	X-linked Severe Combined Immunodeficiency; X-SCID; XSCID	National Institute of Allergy and Infectious Diseases (NIAID)	2025-05-09	PHASE1; PHASE2
NCT06325709	RECRUITING	Chronic Granulomatous Disease (CGD); X-Linked Chronic Granulomatous Disease	National Institute of Allergy and Infectious Diseases (NIAID)	2024-04-17	PHASE1; PHASE2
NCT07605416	RECRUITING	Plasma Cell Leukemia	National Cancer Institute (NCI)	2027-04-20	PHASE2
NCT07775313	NOT_YET_RECRUITING	WHIM; Warts; Hypogammaglobulinemia; Immunodeficiency; Myelokathexis	National Institute of Allergy and Infectious Diseases (NIAID)	2026-09-09	PHASE1; PHASE2
NCT02015013	RECRUITING	Idiopathic CD4-Positive; T-Lymphocytopenia	National Institute of Allergy and Infectious Diseases (NIAID)	2014-01-15	PHASE2
NCT06872333	RECRUITING	Graft Failure; Sickle Cell Disease; Hemoglobinopathies	Masonic Cancer Center, University of Minnesota	2024-11-19	PHASE2

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