Home GPCR & G Protein CXCR antagonist - HIV inhibitor Plerixafor (AMD3100) For research use only.

Plerixafor (AMD3100)

Synonyms: JM 3100, SID791

Plerixafor (AMD3100, JM 3100, SID791) 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. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

Plerixafor (AMD3100) Chemical Structure

Plerixafor (AMD3100) Chemical Structure

CAS: 110078-46-1

Selleck's Plerixafor (AMD3100) has been cited by 95 publications

Purity & Quality Control

Batch: Purity: 99.93%
99.93

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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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Biological Activity

Description Plerixafor (AMD3100, JM 3100, SID791) 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. Plerixafor inhibits human immunodeficiency virus (HIV) replication.
Targets
CXCL12 [1]
(Cell-free assay)		 CXCR4 [1]
(Cell-free assay)
5.7 nM 44 nM
In vitro
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]
Kinase Assay Receptor binding assays
For the competition binding studies against CXCR4, a concentration range of Plerixafor is incubated for 3 hours at 4 °C in binding buffer (PBS containing 5 mM MgCl2, 1 mM Ca Cl2, 0.25% BSA, pH 7.4) with 5 × 105 CCRF–CEM cells and 100 pM 125I-SDF-1α (2200 Ci/mmol) in Milipore DuraporeTM filter plates. Unbound 125I-SDF-1α is removed by washing with cold 50 mM HEPES, 0.5 M NaCl pH 7.4. The competition binding assay against BLT1 is performed on membranes from CHO-S cells expressing recombinant BLT1. The membranes are prepared by mechanical cell lysis followed by high speed centrifugation, re-suspended in 50 mm HEPES, 5 mM MgCl2 buffer and flash frozen. The membrane preparation is incubated with Plerixafor for 1 hour at room temperature in an assay mixture containing 50 mM Tris, pH 7.4, 10 mM MgCl2, 10 mM CaCl2, 4 nM LTB4 mixed with 1 nM 3H-LTB4 (195.0 Ci/mmol) and 8 μg membrane. The unbound 3H-LTB4 is separated by filtration on Millipore Type GF-C filter plates.
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence CXCR4 β-arrestin2 28521261
In Vivo
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]
Animal Research Animal Models Twelve-week-old C57BL/6 mice with segmental bone defect
Dosages 5 mg/kg
Administration Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05343572 Recruiting Asherman Syndrome|Atrophic Endometrium|Recurrent Implantation Failure Hugh Taylor|Yale University November 1 2023 Early Phase 1
NCT05421416 Not yet recruiting Stem Cell Transplant Complications AHS Cancer Control Alberta November 1 2023 Phase 2
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 Magenta Therapeutics Inc.|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 --

Chemical lnformation & Solubility

Molecular Weight 502.78 Formula

C28H54N8
CAS No. 110078-46-1 SDF Download Plerixafor (AMD3100) SDF
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3
Storage (From the date of receipt)

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Ethanol : 100 mg/mL

Water : 15 mg/mL

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


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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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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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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