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AMD3100 (Plerixafor) Antagoniste de CXCR4

Name: AMD3100 (Plerixafor)
Brand: Selleck Chemicals
SKU: S8030
Rating: 5 (110 reviews)

N° Cat.S8030

Le Plerixafor (AMD3100, JM 3100, SID791) est un antagoniste des r de00e9cepteurs de chimiokines pour la chimiotaxie m de00e9di de00e9e par CXCR4 et CXCL12, avec des IC50 de 44 nM et 5,7 nM respectivement dans des essais sans cellules. Le Plerixafor inhibe la r de00e9plication du virus de l'immunod de00e9ficience humaine (HIV).

AMD3100 (Plerixafor) CXCR antagoniste Chemical Structure

Structure chimique

Poids moléculaire: 502.78

Aller à

Contrôle qualité

Lot : Pureté : 99.93%

99.93

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 AMG 487 SX-682 LY2510924 Danirixin (GSK1325756)

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
CHOK1	Function assay			Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00004 μM.	17715128
CHOK1	Function assay			Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00009 μM.	17715128
CHOK1	Function assay			Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50 = 0.00081 μM.	17715128
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM.	17599916
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50 = 0.002 μM.	26974376
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50 = 0.002 μM.	26974376
HEK293	Antiviral 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 = 0.0023 μM.	19451305
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0024 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.003 μM.	17599916
PBMC	Function assay			Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50 = 0.0038 μM.	14698189
MT4	Antiviral 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 = 0.004 μM.	20043638
MT-4	Function assay			Effective concentration against HIV-1(IIIB) replication in MT-4 cells, EC50 = 0.0042 μM.	8568797
HEK293	Antiviral assay		2 days	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0046 μM.	19451305
HEK293	Antiviral assay		2 days	Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0053 μM.	19451305
MT-4	Function assay			Effective concentration against HIV-2(ROD) replication in MT-4 cells, EC50 = 0.0059 μM.	8568797
CEM-CCRF	Function assay		30 mins	Inhibition of PE-conjugated-12G5 anti-CXCR4 antibody binding to CXCR4 in human CEM-CCRF cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis, IC50 = 0.006 μM.	27571038
HEK293	Antiviral assay		2 days	Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0062 μM.	19451305
HEK293	Antiviral assay		2 days	Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.007 μM.	19451305
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.0076 μM.	17599916
MT-4	Antiviral assay			Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound, EC50 = 0.008 μM.	18378713
MT-4	Antiviral assay			Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound, EC50 = 0.008 μM.	18378713
MT-4	Antiviral assay			Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound, EC50 = 0.008 μM.	18378713
HEK293	Antiviral assay		2 days	Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.009 μM.	19451305
HEK293	Antiviral assay		2 days	Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0092 μM.	19451305
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.014 μM.	17599916
MT-4	Antiviral assay			Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.014 μM.	18378713
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.017 μM.	17599916
CD4+ T	Function assay			Antagonist activity at CXCR4 in human CD4+ T cells assessed as inhibition of CXCL12-mediated cytosolic calcium level preincubated with compounds followed by CXCL12 stimulation by calcium 4 dye-based FLIPR assay, IC50 = 0.018 μM.	29494843
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.019 μM.	17599916
MT4	Antiviral assay		5 days	Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine, EC50 = 0.025 μM.	26094944
Jurkat	Function assay			Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration, IC50 = 0.0274 μM.	19188071
MT-4	Antiviral assay			Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound, EC50 = 0.028 μM.	18378713
MT4	Antiviral assay		5 days	Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, EC50 = 0.032 μM.	26094944
MT-4	Antiviral assay			Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.034 μM.	18378713
MT4	Antiviral assay		5 days	Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine, EC50 = 0.039 μM.	26094944
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.046 μM.	17599916
MT-4	Antiviral assay			Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound, EC50 = 0.049 μM.	18378713
MT-4	Antiviral assay			Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound, EC50 = 0.056 μM.	18378713
MT-4	Function assay			Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50 = 0.065 μM.	14698189
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells, IC50 = 0.0727 μM.	19451305
IR983F	Function assay			Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50 = 0.108 μM.	19053768
CEM-SS	Function assay			Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50 = 0.127 μM.	14698189
COS7	Function assay			Antagonist activity at human CXCR4 V196A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.14 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells, IC50 = 0.1437 μM.	19451305
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 H281A mutant expressed in COS7 cells, Ki = 0.16 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 F172A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.17 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells, IC50 = 0.1753 μM.	19451305
COS7	Function assay			Antagonist activity at human CXCR4 H281A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.19 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells, IC50 = 0.1966 μM.	19451305
COS7	Function assay			Antagonist activity at human wild type CXCR4 expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.22 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells, IC50 = 0.2356 μM.	19451305
CEM	Function assay			Displacement of [125I]CXCL12 from CXCR4 in human CEM cells, IC50 = 0.245 μM.	19053768
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells, IC50 = 0.2585 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells, IC50 = 0.259 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells, IC50 = 0.2658 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells, IC50 = 0.2891 μM.	19451305
COS7	Function assay			Antagonist activity at human CXCR4 H203A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM.	17599916
COS7	Function assay			Antagonist activity at transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 T287A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM.	17599916
HPBALL	Function assay		3 hrs	Displacement of 12G5-CXCL12 from CXCR4 in human HPBALL cells after 3 hrs by FACS analysis, IC50 = 0.29 μM.	29494843
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells, IC50 = 0.2964 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells, IC50 = 0.3002 μM.	19451305
CEM-SS	Antiviral assay			Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication, IC50 = 0.32 μM.	19356827
COS7	Function assay			Antagonist activity at human CXCR4 L120F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.33 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 Q200W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.4 μM.	17599916
MT4	Antiviral assay			Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication, IC50 = 0.41 μM.	19356827
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells, IC50 = 0.4695 μM.	19451305
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200A mutant expressed in COS7 cells, Ki = 0.56 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells, IC90 = 0.5722 μM.	19451305
COS7	Function assay			Antagonist activity at human CXCR4 I259W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.63 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 Y255A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.66 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 H113A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.74 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells, IC90 = 0.7956 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells, IC90 = 0.8212 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells, IC90 = 0.8213 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells, IC90 = 0.8606 μM.	19451305
COS7	Function assay			Displacement of [125I]12G5 antibody from human wild type CXCR4 expressed in COS7 cells, Ki = 0.89 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 Q200A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.93 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells, IC90 = 0.9302 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells, IC90 = 0.9711 μM.	19451305
MDA-MB-231	Function assay		10 mins	Displacement of biotinylated TN14003 from CXCR4 CXCL12 binding domain in human MDA-MB-231 cells preincubated for 10 mins followed by biotinylated TN14003 addition measured after 30 mins using streptavidin-conjugated rhodamine by fluorescence microscopic a, EC = 1 μM.	27179215
MDA-MB-231	Function assay		10 mins	Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells preincubated for 10 mins followed by TN14003 addition measured after 30 mins by rhodamine dye-based microscopic analysis, EC = 1 μM.	29529500
MDA-MB-231	Function assay		10 mins	Displacement of biotinylated-TN14003 from CXCR4 in human MDA-MB-231 cells assessed as reduction in fluorescence preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based microscopic , EC = 1 μM.	27914361
MDA-MB-231	Function assay		10 mins	Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells assessed as reduction in fluorescence preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based immunofl, EC = 1 μM.	28521261
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 I284A mutant expressed in COS7 cells, Ki = 1.1 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 I284A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 1.2 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells, Ki = 1.5 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 H203A mutant expressed in COS7 cells, Ki = 1.8 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 D171N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 1.8 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 3 of human CXCR4 H113A mutant expressed in COS7 cells, Ki = 2 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D262N mutant, IC50 = 2.541 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D171ND262N mutant, IC50 = 2.694 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200W mutant expressed in COS7 cells, Ki = 2.7 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207F mutant expressed in COS7 cells, Ki = 2.7 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207W mutant expressed in COS7 cells, Ki = 3 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 T287A mutant expressed in COS7 cells, Ki = 3.1 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F174A mutant expressed in COS7 cells, Ki = 3.2 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D182A mutant expressed in COS7 cells, Ki = 3.2 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y256A mutant expressed in COS7 cells, Ki = 4 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 N176A mutant expressed in COS7 cells, Ki = 4.1 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 V196A mutant expressed in COS7 cells, Ki = 4.6 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259W mutant expressed in COS7 cells, Ki = 4.6 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F172A mutant expressed in COS7 cells, Ki = 4.7 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 D262N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 4.7 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 S263A mutant expressed in COS7 cells, Ki = 5.4 μM.	17599916
CCRF-CEM	Function assay		30 mins	Inhibition of anti-CXCR4 PE antibody clone 12G5 binding to CXCR4 in human CCRF-CEM cells preincubated for 30 mins followed by anti-CXCR4 PE antibody clone 12G5 addition measured after 30 mins by flow cytometric method, IC50 = 6.2 μM.	29125295
COS7	Function assay			Antagonist activity at human CXCR4 E288A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 6.4 μM.	17599916
MT4	Cytotoxicity assay			Cytotoxicity against human MT4 cells by MTT assay, CC50 = 6.5 μM.	19356827
COS7	Function assay			Antagonist activity at human CXCR4 A175F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 8.5 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y255A mutant expressed in COS7 cells, Ki = 9.7 μM.	17599916
MT-4	Function assay			Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells, EC50 = 10 μM.	9925728
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 D171N mutant expressed in COS7 cells, Ki = 13 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D187A mutant expressed in COS7 cells, Ki = 14 μM.	17599916
HL60	Function assay			Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50 = 15.2 μM.	19188071
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 A175F mutant expressed in COS7 cells, Ki = 36 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 D262N mutant expressed in COS7 cells, Ki = 46 μM.	17599916
COS, TZM-bl	Function assay			Inhibition of HIV1 NL4-3 envelope glycoprotein 120-mediated membrane fusion between virus-transfected african green monkey COS cells and human TZM-bl cells by luciferase-based cell-cell fusion assay in presence of IC9564	17954689
CXCR4+/CD4+/U87	Function assay			Inhibition of HIV1 92TH594 infected CXCR4+/CD4+/U87 cells to assess co-receptor tropism as luciferase activity	17116663
CXCR4+/CD4+/U87	Function assay			Inhibition of HIV1 HXB2 infected CXCR4+/CD4+/U87 cells to assess co-receptor tropism as luciferase activity	17116663
U87	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
CHOK1	Function assay			Induction of [125I]MCP1 dissociation from CCR2/CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay	17715128
CHOK1	Function assay			Antagonist activity at CXCR4 expressed in CHOK1 cells assessed as inhibition of SDF1-alpha-induced signaling by aequorin-based assay	17715128
CHOK1	Function assay			Antagonist activity at CCR2/CXCR4 expressed in CHOK1 cells assessed as inhibition of SDF1-alpha-induced signaling by aequorin-based assay	17715128
CHOK1	Function assay			Induction of [125I]SDF1alpha dissociation from CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay	17715128
U87.CD4	Function assay			Antagonist activity at human CXCR4 H281A mutant expressed in U87.CD4 cells assessed as inhibition of CXCL12-induced calcium mobilization	17599916
MT2	Antiviral 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
MOLT4	Function assay	1000 nM		Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis	19451305
TZM-bl	Antiviral assay	100 uM	24 hrs	Antiviral activity against HIV NL-Lai infected in human TZM-bl cells assessed as inhibition of viral infection at 100 uM treated before viral infection measured after 24 hrs by luciferase assay	21783371
Jurkat	Function assay	0.01 to 100 uM		Inhibition of CXCR4 in human Jurkat cells assessed as reduction in HIV-Nef-M1-induced mitochondrial membrane depolarization at 0.01 to 100 uM by JC1 dye based fluorescence depolarization assay	26191361
MDA-MB-231	Function assay	100 nM	24 hrs	Antagonist activity at CXCR4-mediated chemotaxis in human MDA-MB-231 cells assessed as inhibition of CXCL12-induced cell invasion at 100 nM after 24 hrs by crystal violet staining-based microscopic matrigel assay	29494843
TZM-bl	Antiviral assay		1 hr	Antiviral activity against HIV1 HXB2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral entry treated 1 hr post infection measured after 48 hrs by luciferase reporter gene assay	28266845
CXCR4+	Function assay	6 mg/kg	2 hrs	Induction hematopoietic stem cell mobilization in C57BL/6 mouse assessed as increase in CXCR4+ cells in blood at 6 mg/kg, sc measured after 2 hrs by APC-conjugated anti-CXCR4-staining based flow cytometry relative to vehicle control	29314840
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Informations chimiques, stockage et stabilité

Poids moléculaire	502.78	Formule	C₂₈H₅₄N₈	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	110078-46-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	JM 3100, SID791			Smiles	C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3

Solubilité

In vitro
Lot:

Ethanol : 100 mg/mL

Water : 15 mg/mL

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

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Masse	Concentration	Volume	Poids moléculaire
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In vivo Lot:
Clear solution	5%absolute ethyl alcohol 1 40% PEG 300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.100mg/ml (2.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml absolute ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% ethyl alcohol 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	0.100mg/ml (0.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 mg/ml clear ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

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

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny 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 dabord 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, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

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

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	CXCL12 (Cell-free assay) 5.7 nM CXCR4 (Cell-free assay) 44 nM
In vitro	Le Plerixafor (AMD3100) inhibe la chimiotaxie m de00e9di de00e9e par CXCL12 avec une puissance l de00e9g de00e8rement meilleure que son affinit de00e9 pour CXCR4. Il antagonise de00e9galement la liaison du ligand SDF-1/CXCL12 avec un IC50 de 651 nM. Ce compos de00e9 inhibe la liaison de GTP m de00e9di de00e9e par SDF-1, le flux calcique m de00e9di de00e9 par SDF-1 et la chimiotaxie stimul de00e9e par SDF-1 avec des IC50 de 27 nM, 572 nM et 51 nM, respectivement. Il n'inhibe pas le flux calcique contre les cellules exprimant CXCR3, CCR1, CCR2b, CCR4, CCR5 ou CCR7 lorsqu'elles sont stimul de00e9es avec leurs ligands sp de00e9cifiques, et il n'inhibe pas non plus la liaison du r de00e9cepteur de00e0 LTB4. de00c0 lui seul, il n'induit pas de flux calcique dans les cellules CCRF du2013CEM, qui expriment plusieurs GPCR & G Protein, dont CXCR4, CCR4 et CCR7.
Kinase Assay	Essais de liaison r de00e9cepteur
Kinase Assay	Pour les de00e9tudes de liaison comp de00e9titive contre CXCR4, le Plerixafor (AMD3100) est incub de00e9 de00e0 une gamme de concentrations pendant 3 heures de00e0 4 de202f de00b0C dans un tampon de liaison (PBS contenant 5 de202f mM de MgCl₂, 1 de202f mM de CaCl₂, 0,25% de BSA, pH de202f 7,4) avec 5 de202f de00d7 de202f 10⁵ cellules CCRF du2013CEM et 100 de202f pM de ¹²⁵I-SDF-1 de03b1 (2200 de202f Ci/mmol) dans des plaques filtrantes Milipore Durapore^TM. Le ¹²⁵I-SDF-1 de03b1 non li de00e9 est de00e9limin de00e9 par lavage avec 50 de202f mM de HEPES froid, 0,5 de202f M de NaCl pH de202f 7,4. L'essai de liaison comp de00e9titive contre BLT1 est r de00e9alis de00e9 sur des membranes de cellules CHO-S exprimant BLT1 recombinant. Les membranes sont pr de00e9par de00e9es par lyse cellulaire m de00e9canique suivie d'une centrifugation de00e0 haute vitesse, resuspendues dans un tampon de 50 de202f mM de HEPES, 5 de202f mM de MgCl₂ et congel de00e9es rapidement. Ce compos de00e9 est incub de00e9 avec la pr de00e9paration membranaire pendant 1 heure de00e0 temp de00e9rature ambiante dans un m de00e9lange d'essai contenant 50 de202f mM de Tris, pH de202f 7,4, 10 de202f mM de MgCl₂, 10 de202f mM de CaCl₂, 4 de202f nM de LTB₄ m de00e9lang de00e9 avec 1 de202f nM de ³H-LTB₄ (195,0 de202f Ci/mmol) et 8 de202f de03bcg de membrane. Le ³H-LTB₄ non li de00e9 est s de00e9par de00e9 par filtration sur des plaques filtrantes Millipore Type GF-C.
In vivo	Chez les souris diab de00e9tiques, une seule application topique de Plerixafor (AMD3100) favorise la cicatrisation des plaies en augmentant la production de cytokines, en mobilisant les EPC de la moelle osseuse et en am de00e9liorant l'activit de00e9 des fibroblastes et des monocytes/macrophages, augmentant ainsi l'angiogen de00e8se et la vasculogen de00e8se. Des cohortes de souris re de00e7oivent du PBS, de l'IGF1, du PDGF, du SCF ou du VEGF pendant cinq jours cons de00e9cutifs et ce compos de00e9 le 5e jour. Le nombre et la taille des colonies sont les plus de00e9lev de00e9s chez les souris inject de00e9es avec IGF1 plus le compos de00e9 par rapport aux groupes trait de00e9s avec PDGF, SCF et VEGF, en combinaison avec 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

Méthodes	Biomarqueurs	Images	PMID
Immunofluorescence	β-arrestin2 CXCR4		31186083

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	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\|Autologous Stem Cell Transplantation\|Leukapheresis	Fondazione Policlinico Universitario Agostino Gemelli IRCCS	January 1 2022	--

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

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Questions fréquemment posées

Question 1:
How about the half-life of it (Cat S8030)?

Réponse :
Its biological half-life is 3-5 hours: https://en.wikipedia.org/wiki/Plerixafor.

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