Cat. No.: HY-10046

Plerixafor

(Synonyms: AMD 3100; JM3100; SID791)

106 Cited Publications

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Based on 106 publication(s) in Google Scholar

Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM.

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 110078-46-1
Formula: C₂₈H₅₄N₈
Molecular Weight:502.78

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Plerixafor Chemical Structure

CAS No.: 110078-46-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (106)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target^[3]^[7]

¹²⁵I-CXCL12-CXCR4

44 nM (IC₅₀)

¹²⁵I-CXCL12-CXCR7

HIV-1

1-10 nM (EC₅₀)

HIV-2

1-10 nM (EC₅₀)

All CXCR Isoforms :

All HIV Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	245 nM Compound: AMD-3100	Displacement of [125I]CXCL12 from CXCR4 in human CEM cells Displacement of [125I]CXCL12 from CXCR4 in human CEM cells	[PMID: 19053768]
CEM-SS	CC₅₀	>10 μM Compound: AMD-3100	Concentration of compound causing 50% death of uninfected cells Concentration of compound causing 50% death of uninfected cells	[PMID: 14698189]
CEM-SS	CC₅₀	>5 μM Compound: AMD-3100	Cytotoxicity against human CEM-SS cells by MTT assay Cytotoxicity against human CEM-SS cells by MTT assay	[PMID: 19356827]
CEM-SS	EC₅₀	0.127 μM Compound: AMD-3100	Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells	[PMID: 14698189]
CEM-SS	IC₅₀	0.32 μM Compound: AMD-3100	Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication	[PMID: 19356827]
CHO	IC₅₀	0.051 μM Compound: AMD3100	Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis	[PMID: 30978562]
CHO	IC₅₀	65 nM Compound: AMD3100	Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay	[PMID: 27658790]
CHO-K1	IC₅₀	0.04 nM Compound: AMD-3100	Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells	[PMID: 17715128]
CHO-K1	IC₅₀	0.09 nM Compound: AMD-3100	Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells	[PMID: 17715128]
CHO-K1	IC₅₀	0.81 nM Compound: AMD-3100	Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells	[PMID: 17715128]
GHOST CCR5	IC₅₀	>5 μM Compound: AMD-3100	Inhibitory concentration of compound against HIV-1 Ba1 strain in GHOST CCR5 cell line Inhibitory concentration of compound against HIV-1 Ba1 strain in GHOST CCR5 cell line	[PMID: 14698189]
GHOST CXCR4	IC₅₀	0.00095 μM Compound: AMD-3100	Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line	[PMID: 14698189]
HEK293	IC₅₀	>1000 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 D171A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 D171A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	>1000 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 D262A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 D262A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	>1000 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 E288A/L290A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 E288A/L290A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	143.7 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	175.3 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	196.6 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	2.3 nM Compound: AMD-3100	Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	213.1 nM Compound: 1; AMD3100	Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method	[PMID: 29314840]
HEK293	IC₅₀	235.6 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	258.5 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	259 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	265.8 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	289.1 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	296.4 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	300.2 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	4.6 nM Compound: AMD-3100	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	469.5 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	5.3 nM Compound: AMD-3100	Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	6.2 nM Compound: AMD-3100	Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	7 nM Compound: AMD-3100	Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	72.7 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	9 nM Compound: AMD-3100	Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	9.2 nM Compound: AMD-3100	Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HL-60	IC₅₀	15.2 μM Compound: 1, AMD-3100	Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells	[PMID: 19188071]
HuT78	CC₅₀	241 μM Compound: 1	Cellular cytotoxicity against HUT-78 cells. Cellular cytotoxicity against HUT-78 cells.	[PMID: 7562918]
Jurkat	IC₅₀	27.4 nM Compound: 1, AMD-3100	Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration	[PMID: 19188071]
MT4	CC₅₀	>10 μg/mL Compound: AMD-3100	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 23157587]
MT4	CC₅₀	>10 μM Compound: AMD-3100	Concentration of compound causing 50% death of uninfected cells Concentration of compound causing 50% death of uninfected cells	[PMID: 14698189]
MT4	CC₅₀	>421 μM Compound: 1, AMD-3100	Cytotoxicity against human MT4 cells after 4 days by MTT method Cytotoxicity against human MT4 cells after 4 days by MTT method	[PMID: 20043638]
MT4	CC₅₀	>421 μM Compound: 10d	Concentration required to reduce the viability of mock infected cells by 50% Concentration required to reduce the viability of mock infected cells by 50%	[PMID: 8568797]
MT4	CC₅₀	>50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 26094944]
MT4	CC₅₀	>50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine	[PMID: 26094944]
MT4	CC₅₀	>50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine	[PMID: 26094944]
MT4	CC₅₀	>50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine	[PMID: 26094944]
MT4	CC₅₀	>50 μM Compound: AMD3100	Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	[PMID: 32305183]
MT4	CC₅₀	>50 μM Compound: AMD3100	Cytotoxicity against in human MT-4 after 5 days by MTT assay Cytotoxicity against in human MT-4 after 5 days by MTT assay	[PMID: 33316719]
MT4	CC₅₀	50 μM Compound: 37	Concentration required to cause 50% death of uninfected MT-4 cells Concentration required to cause 50% death of uninfected MT-4 cells	[PMID: 9925728]
MT4	CC₅₀	6.5 μM Compound: AMD-3100	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 19356827]
MT4	EC₅₀	0.004 μM Compound: 1, AMD-3100	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay	[PMID: 20043638]
MT4	EC₅₀	0.0042 μM Compound: 10d	Effective concentration against HIV-1(IIIB) replication in MT-4 cells Effective concentration against HIV-1(IIIB) replication in MT-4 cells	[PMID: 8568797]
MT4	EC₅₀	0.0059 μM Compound: 10d	Effective concentration against HIV-2(ROD) replication in MT-4 cells Effective concentration against HIV-2(ROD) replication in MT-4 cells	[PMID: 8568797]
MT4	EC₅₀	0.008 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.008 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.008 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.014 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.025 μM Compound: AMD3100	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 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	[PMID: 26094944]
MT4	EC₅₀	0.028 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.032 μM Compound: AMD3100	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 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	[PMID: 26094944]
MT4	EC₅₀	0.034 μM Compound: AMD3100	Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.039 μM Compound: AMD3100	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 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	[PMID: 26094944]
MT4	EC₅₀	0.049 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.056 μM Compound: AMD3100	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 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	[PMID: 18378713]
MT4	EC₅₀	0.065 μM Compound: AMD-3100	Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells	[PMID: 14698189]
MT4	EC₅₀	10 μM Compound: 37	Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells	[PMID: 9925728]
MT4	EC₅₀	2 nM Compound: AMD3100; 15c; 16c	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 26974376]
MT4	EC₅₀	2 nM Compound: AMD3100; 15c; 16c	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 26974376]
MT4	IC₅₀	0.017 μg/mL Compound: AMD-3100	Antiviral activity against X4 HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of viral replication pre-incubated for 30 mins measured 5 days post infection by MTT assay Antiviral activity against X4 HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of viral replication pre-incubated for 30 mins measured 5 days post infection by MTT assay	[PMID: 23157587]
MT4	IC₅₀	0.41 μM Compound: AMD-3100	Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication	[PMID: 19356827]
MT4	IC₅₀	1.5 ng/mL Compound: AMD-3100	Antiviral activity against HIV1 NL4.3 in human MT4 cells Antiviral activity against HIV1 NL4.3 in human MT4 cells	[PMID: 17452489]
PBMC	CC₅₀	>10 μg/mL Compound: AMD-3100	Cytotoxicity against human PBMC cells by MTT assay Cytotoxicity against human PBMC cells by MTT assay	[PMID: 23157587]
PBMC	CC₅₀	>10 μM Compound: 1a, AMD-3100	Cytotoxicity against PBMC Cytotoxicity against PBMC	[PMID: 17000109]
PBMC	CC₅₀	>10 μM Compound: AMD-3100	Concentration of compound causing 50% death of uninfected cells Concentration of compound causing 50% death of uninfected cells	[PMID: 14698189]
PBMC	EC₅₀	0.0038 μM Compound: AMD-3100	Effective concentration of compound against HIV-1 89.6 strain in PBMC cells Effective concentration of compound against HIV-1 89.6 strain in PBMC cells	[PMID: 14698189]

In Vitro

The CXCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC₅₀, 5.7 nM) with a potency slightly better than its affinity for CXCR4. Plerixafor interferes with the interaction of CXCR4 with its natural ligand, SDF-1 (CXCL12). Treating the cells with CCX771 or CXCL11 has no effect on CXCL12-mediated MOLT-4 or U937 TEM. In contrast, 10 μM Plerixafor inhibits CXCL12-mediated TEM in both cells lines^[1]
. Plerixafor prevents the infiltration of tumor-associated macrophages (TAMs) into the tumor tissues^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Plerixafor (2 mg/kg) administration to UUO mice exacerbates renal interstitial T cell infiltration, resulting in increased production of the pro-inflammatory cytokines IL-6 and IFN-γ and decreased expression of the anti-inflammatory cytokine IL-10^[5].
Both perivascular and interstitial fibrosis are significantly reduced by the CXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks^[6]. LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 110078-46-1
Appearance Solid
Molecular Weight 502.78
Formula C₂₈H₅₄N₈
Color White to off-white
SMILES

C1(CN2CCCNCCNCCCNCC2)=CC=C(C=C1)CN3CCNCCCNCCNCCC3
Synonyms

AMD 3100; JM3100; SID791
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (106)

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Journal Impact Factor

Immunity

Small-molecule CBP/p300 histone acetyltransferase inhibition mobilizes leukocytes from the bone marrow via the endocrine stress response. [Abstract]

2024 Feb 13;57(2):364-378.e9. PMID: 38301651
Cell Stem Cell

Engineered MSCs enable bone marrow-targeted immunomodulation. [Abstract]

2026 Apr 2;33(4):660-675.e5. PMID: 41895281
Bioact Mater

Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering. [Abstract]

2021 Jan 7;6(7):2039-2057. PMID: 33511306

Plerixafor purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]

Western blot analysis of the expression of CXCR4, integrin αvβ3, p-Jak2, Jak2, p-FAK, FAK, p-STAT3 and STAT3 in MSCs (pretreated with a CXCR4 inhibitor (AMD3100; 20 μM; pretreated with 1 h) and an integrin αvβ3 inhibitor (cyclo(-RGDfK))) after the addition of 152RM for 24 h.
Cell Mol Immunol

NLRP3-dependent pyroptosis is required for HIV-1 gp120-induced neuropathology. [Abstract]

2020 Mar;17(3):283-299. PMID: 31320730

Plerixafor purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2020 Mar;17(3):283-299. [Abstract]

ELISA of IL-1β in supernatants of BV2 cells stimulated with gp120 LAV (0.5 μg/mL) for 24 h in the presence of increasing doses of a CXCR4-specific inhibitor (AMD3100, 0.1-10 μM; prestimulated with 30 min-2 h).
Nat Cell Biol

Trafficking circuit of CD8+ T cells between the intestine and bone marrow governs antitumour immunity. [Abstract]

2024 Aug;26(8):1346-1358. PMID: 39039181
Adv Funct Mater

2025 Dec 16.
Adv Funct Mater

2024 Dec 23.
Adv Funct Mater

2020, 2000309.

Plerixafor purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2020, 2000309.

NOD/SCID mice were i.p. injected with AMD3100 (4 mg/kg). After 1 h, the mice are i.v. injected with iFluor 647-labeled Aazo@CMSN. At 12 h after nanoparticle injection, the mouse craniums are excised for the observation of nanoparticle bone marrow niches targeting under CLSM. Pre-treatment with AMD3100 significantly declined the bone marrow niches targeting of the nanoparticles.
Nat Commun

Nef stabilizes actin to prevent HIV-1 sensing by RIG-I-like receptors. [Abstract]

2025 Dec 7;16(1):10945. PMID: 41354661
Bone Res

Neonatal bone marrow interstitial fluid supports expansion and osteogenic ability of human bone marrow mesenchymal stromal cells. [Abstract]

2025 Dec 15;13(1):102. PMID: 41392038
Adv Sci (Weinh)

Nanoparticle-Mediated CXCL12-CXCR4 Inhibition Reprograms Macrophages and Suppresses Gastric Carcinoma. [Abstract]

2025 Jun 19:e00225. PMID: 40536774
Leukemia

Distinct stromal cell populations define the B-cell acute lymphoblastic leukemia microenvironment. [Abstract]

2025 Aug 15. PMID: 40817406

Plerixafor purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Aug 15. [Abstract]

Effect of cytokine signaling blockade on ALL cell survival in co-culture with stromal populations. ALL cells were co-cultured with early mesenchymal progenitors, adipogenic progenitors, or cultured alone. Cell survival was assessed after treatment with blocking antibodies against IL7, Osteopontin, or the CXCR4 inhibitor Plerixafor (1 nM; 7 days), Mouse IgG1 kappa, Isotype Control (1 ug/mL; 7 days).
Cardiovasc Res

Periaortic lymphatic vessels protect against thoracic aortic dissection through mobilizing immune response. [Abstract]

2025 Nov 11:cvaf215. PMID: 41213294
Theranostics

CXCL12-mediated HOXB5 overexpression facilitates Colorectal Cancer metastasis through transactivating CXCR4 and ITGB3. [Abstract]

2021 Jan 1;11(6):2612-2633. PMID: 33456563

Plerixafor purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633. [Abstract]

Caco-2 cells are incubated with vehicle or AMD3100 (1 µg/ml, 24 hours) after lentivirus transfection (LV-HOXB5), then Western blotting assays are conducted to measure the protein levels of CXCL12, HOXB5, CXCR4, p-ERK and p-ETS1 in the indicated cell lines.

Plerixafor purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633. [Abstract]

Transwell assays indicated that AMD3100 treatment (1 µg/ml, 24 hours) significantly decreases the migration and invasion of Caco-2-HOXB5 cells.
Chem Eng J

2025 Oct 15.
Biomaterials

Engineered cell membrane vesicles loaded with lysosomophilic drug for acute myeloid leukemia therapy via organ-cell-organelle cascade-targeting. [Abstract]

2025 Jan 3:317:123091. PMID: 39778270
J Nanobiotechnology

CXCR4-engineered fibroblast membrane nanovesicles for Photothermal-enhanced ferroptotic therapy through chemokine-navigated tumor homing. [Abstract]

2025 Dec 30;24(1):102. PMID: 41462305
J Nanobiotechnology

The bone marrow mesenchymal stem cells derived migrasomes induced by Titania nanotubes surface serve as chemotaxis effect for osteogenesis. [Abstract]

2025 Aug 29;23(1):592. PMID: 40877924
Nano Today

2022, 47: 101689.
Research (Wash D C)

2026 Mar 19.
Cell Rep Med

Augment proteasome inhibitor efficacy activates CD8+ T cell-mediated antitumor immunity in breast cancer. [Abstract]

2025 Jul 15;6(7):102211. PMID: 40609539
J Immunother Cancer

Natural lung-tropic TH9 cells: a sharp weapon for established lung metastases. [Abstract]

2024 Dec 4;12(12):e009629. PMID: 39631847
Mater Today Bio

Nanoparticles coated with osteoblast-like cell membranes as curcumin delivery vehicles for targeted postmenopausal osteoporosis therapy. [Abstract]

2025 Dec 9:36:102636. PMID: 41497898
Mater Today Bio

A biomimetic targeted nanosystem delivering synergistic inhibitors for glioblastoma immune microenvironment reprogramming and treatment. [Abstract]

2024 Sep 1:28:101222. PMID: 39296357
J Neuroinflammation

CXCR4 and CXCR6 dually limit T cell entry into the polyomavirus-infected brain. [Abstract]

2025 Jun 28;22(1):169. PMID: 40581668
Cancer Lett

CXCR4 inhibitor, AMD3100, down-regulates PARP1 expression and Synergizes with olaparib causing severe DNA damage in BRCA-proficient triple-negative breast cancer. [Abstract]

2022 Oct 7;551:215944. PMID: 36209974

Plerixafor purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944. [Abstract]

Viability of cells treated with combinations different concentrations of AMD3100 and Olaparib for 24 h.

Plerixafor purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944. [Abstract]

Immunohistochemical staining of proliferation-related protein, Ki-67, in breast cancer after treatment with control, AMD3100 (2.5 mg/kg), Olaparib, or a combination of AMD3100 and Olaparib.
Int J Biol Sci

SDF-1 in Mammary Fibroblasts of Bovine with Mastitis Induces EMT and Inflammatory Response of Epithelial Cells. [Abstract]

2017 May 5;13(5):604-614. PMID: 28539833

Plerixafor purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 May 5;13(5):604-614. [Abstract]

Epithelial cells with or without AMD3100 pretreatment are cultured in conditioned medium (CM) from LPS-treated NFs or LTA-treated NFs for 3 days, and the secretion of TNF-α in the supernatant of culture is detected by ELISA. Epithelial cells cultured in MSM are used as control. Both LPS-treated NFs and LTA-treated NFs enhanced the section of TNF-α by epithelial cells compared with control. Pretreatment of epithelial cells with AMD3100 significantly attenuates the increase of TNF-α.
Acta Biomater

Chemotactic recruitment of genetically engineered cell membrane-camouflaged metal-organic framework nanoparticles for ischemic osteonecrosis treatment. [Abstract]

2024 Jul 17:S1742-7061(24)00395-7. PMID: 39029641
Acta Biomater

Nanoparticle-mediated blockade of CXCL12/CXCR4 signaling enhances glioblastoma immunotherapy: Monitoring early responses with MRI radiomics. [Abstract]

2024 Mar 15:177:414-430. PMID: 38360292
Cell Death Dis

TREM2 deficiency in microglia accelerates photoreceptor cell death and immune cell infiltration following retinal detachment. [Abstract]

2023 Mar 28;14(3):219. PMID: 36977680
Cell Death Dis

PGK1 contributes to tumorigenesis and sorafenib resistance of renal clear cell carcinoma via activating CXCR4/ERK signaling pathway and accelerating glycolysis. [Abstract]

2022 Feb 4;13(2):118. PMID: 35121728

Plerixafor purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 4;13(2):118. [Abstract]

PGK1 induced the CXCR4-mediated phosphorylation of AKT (p-AKT) and ERK (p-ERK), and blockade of CXCR4 signaling by AMD3100 (48 h) treatment did not alter cellular PGK1 expression in KIRC cells.
Cell Death Dis

Hepatitis B virus X protein promotes the stem-like properties of OV6+ cancer cells in hepatocellular carcinoma. [Abstract]

2017 Jan 19;8(1):e2560. PMID: 28102846
Proc Natl Acad Sci U S A

Structural mechanisms underlying the modulation of CXCR4 by diverse small-molecule antagonists. [Abstract]

2025 Mar 18;122(11):e2425795122. PMID: 40063796
Acta Pharmacol Sin

Lung memory B cells ameliorate Alzheimer's disease-like pathology in 5×FAD mice through the CXCL12-CXCR4 axis. [Abstract]

2025 Oct 17. PMID: 41107404
Phytomedicine

Wikstrol B reactivates latent human immunodeficiency virus (HIV-1) via the nuclear factor-κB (NF-κB) pathway. [Abstract]

2025 Jun:141:156667. PMID: 40233507
Brain Behav Immun

Ds-HMGB1 and fr-HMGB induce depressive behavior through neuroinflammation in contrast to nonoxid-HMGB1. [Abstract]

2017 Jan:59:322-332. PMID: 27647532
J Transl Med

BM-MSCs display altered gene expression profiles in B-cell acute lymphoblastic leukemia niches and exert pro-proliferative effects via overexpression of IFI6. [Abstract]

2023 Sep 5;21(1):593. PMID: 37670388
Biomed Pharmacother

Bone marrow mesenchymal stem cells in microenvironment transform into cancer-associated fibroblasts to promote the progression of B-cell acute lymphoblastic leukemia. [Abstract]

2020 Oct:130:110610. PMID: 34321159
Oncogene

CXCR4 and CXCR7 signaling promotes tumor progression and obesity-associated epithelial-mesenchymal transition in prostate cancer cells. [Abstract]

2022 Oct;41(41):4633-4644. PMID: 36088505
Oncogene

PDGFR-induced autocrine SDF-1 signaling in cancer cells promotes metastasis in advanced skin carcinoma. [Abstract]

2019 Jun;38(25):5021-5037. PMID: 30874597

Plerixafor purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037. [Abstract]

IF staining of the tumor tissue sections showed decreased Ki67 and a reversal of EMT markers indicated by increased E-cadherin and decreased N-cadherin expression in the AMD3100 (5 mg/kg or 3.5 mg/kg) treated groups.

Plerixafor purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037. [Abstract]

Additional EMT-related proteins (Snail and Slug) are downregulated by AMD3100 (5 mg/kg or 3.5 mg/kg) in tumor samples from both diet groups, as quantified by immunoblotting.
Cell Death Discov

CXCL12 alone is enough to Reprogram Normal Fibroblasts into Cancer-Associated Fibroblasts. [Abstract]

2025 Apr 8;11(1):156. PMID: 40199862
Fertil Steril

Protein kinase CK2 participates in estrogen-mediated endothelial progenitor cell homing to endometriotic lesions through stromal cells in a stromal cell-derived factor-1- CXCR4-dependent manner. [Abstract]

2020 May;113(5):1067-1079.e5. PMID: 32386617
Int J Nanomedicine

Co-Delivery Nanomicelles for Potentiating TNBC Immunotherapy by Synergetically Reshaping CAFs-Mediated Tumor Stroma and Reprogramming Immunosuppressive Microenvironment. [Abstract]

2023 Jul 31:18:4329-4346. PMID: 37545872
Cell Mol Life Sci

Crosstalk between purinergic receptor P2Y11 and chemokine receptor CXCR7 is regulated by CXCR4 in human macrophages. [Abstract]

2024 Mar 13;81(1):132. PMID: 38472446
Mol Ther Nucleic Acids

Mechanical stimuli-induced CCL2 restores adult mouse cells to regenerate hair follicles. [Abstract]

2023 Mar 10:32:94-110. PMID: 37020681
J Mater Chem B

Alginate-aker injectable composite hydrogels promoted irregular bone regeneration through stem cell recruitment and osteogenic differentiation. [Abstract]

2018 Apr 7;6(13):1951-1964. PMID: 32254361
Biochem Pharmacol

Targeting the CXCR7 pathway with TC14012 to inhibit endothelial necroptosis and lung cancer metastasis. [Abstract]

2025 Jun:236:116852. PMID: 40049294
Pharmaceutics

Development and Evaluation of 1'-Acetoxychavicol Acetate (ACA)-Loaded Nanostructured Lipid Carriers for Prostate Cancer Therapy. [Abstract]

2021 Mar 24;13(4):439. PMID: 33804975
Cells

Extracellular Vesicles Derived from Bone Marrow in an Early Stage of Ionizing Radiation Damage Are Able to Induce Bystander Responses in the Bone Marrow. [Abstract]

2022 Jan 4;11(1):155. PMID: 35011718
Cells

Tumor Angiogenic Inhibition Triggered Necrosis (TAITN) in Oral Cancer. [Abstract]

2019 Jul 22;8(7):761. PMID: 31336612
Drug Des Devel Ther

Inhibition of CXCR4 in Spinal Cord and DRG with AMD3100 Attenuates Colon-Bladder Cross-Organ Sensitization. [Abstract]

2022 Jan 6;16:67-81. PMID: 35023903
Int J Mol Sci

PIEZO1 Promotes the Migration of Endothelial Cells via Enhancing CXCR4 Expression under Simulated Microgravity. [Abstract]

2024 Jul 1;25(13):7254. PMID: 39000362
Int J Mol Sci

Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET. [Abstract]

2024 May 4;25(9):5018. PMID: 38732237
Int J Mol Sci

Inhibition of Cxcr4 Disrupts Mouse Embryonic Palatal Mesenchymal Cell Migration and Induces Cleft Palate Occurrence. [Abstract]

2023 Aug 13;24(16):12740. PMID: 37628919
Biomolecules

Impact of SDF-1 and AMD3100 on Hair Follicle Dynamics in a Chronic Stress Model. [Abstract]

2024 Sep 25;14(10):1206. PMID: 39456139
Int Immunopharmacol

Apelin-13 regulated thrombotic inflammation and induced homing of EPCs to promote the dissolution and recanalization of deep vein thrombosis. [Abstract]

2025 Dec 13:169:115969. PMID: 41391282
Invest Ophthalmol Vis Sci

CXCR4-Mediated Chemokine Signaling Orchestrates the Progression of Conjunctival Melanocytic Lesions. [Abstract]

2025 Aug 1;66(11):23. PMID: 40778698
Am J Physiol Cell Physiol

Mechanistic insights into SENP1 and OCT4 interaction in promoting drug resistance and stem cell features in colon cancer. [Abstract]

2025 Apr 1;328(4):C1260-C1278. PMID: 40063360
Int Immunopharmacol

Isoferulic acid regulates CXCL12/CXCR4-mediated apoptosis and autophagy in podocyte and mice with STZ-induced diabetic nephropathy. [Abstract]

2024 Nov 30:144:113707. PMID: 39616856
RSC Adv

A multi-stage computational pipeline and in vitro validation for the discovery of small-molecule translation inhibitors targeting the bacterial ribosome. [Abstract]

2026 Apr 7;16(20):18359-18373. PMID: 41953617
Transl Stroke Res

SDF-1α/CXCR4 Pathway Mediates Hemodynamics-Induced Formation of Intracranial Aneurysm by Modulating the Phenotypic Transformation of Vascular Smooth Muscle Cells. [Abstract]

2022 Apr;13(2):276-286. PMID: 34173205
J Cell Mol Med

Stromal Cell Derived Factor-1 Promotes Hepatic Insulin Resistance via Inhibiting Hepatocyte Lipophagy. [Abstract]

2025 Jan;29(2):e70352. PMID: 39855896
J Periodontol

Stromal cell-derived factor-1 regulates expression of vascular endothelial growth factor and osteopontin after tooth extraction. [Abstract]

2025 Jul 8. PMID: 40627767
ACS Infect Dis

Bcl-2 Antagonist Obatoclax Reactivates Latent HIV-1 via the NF-κB Pathway and Induces Latent Reservoir Cell Apoptosis in Latently Infected Cells. [Abstract]

2023 Nov 10;9(11):2105-2118. PMID: 37796279
Br J Haematol

CXCR4 antagonists disrupt leukaemia-meningeal cell adhesion and attenuate chemoresistance. [Abstract]

2023 May;201(3):459-469. PMID: 36535585
Cell Signal

CXCL12-CXCL4 heterodimerization prevents CXCL12-driven breast cancer cell migration. [Abstract]

2020 Feb;66:109488. PMID: 31785332
Mol Med Rep

AMD3100 and SDF‑1 regulate cellular functions of endothelial progenitor cells and accelerate endothelial regeneration in a rat carotid artery injury model. [Abstract]

2020 Oct;22(4):3201-3212. PMID: 32945467
Andrology

Saxagliptin alleviates erectile dysfunction through increasing stromal cell-derived factor-1 in diabetes mellitus. [Abstract]

2023 Feb;11(2):295-306. PMID: 36113503
BMC Complement Altern Med

Baicalin promotes apoptosis and inhibits proliferation and migration of hypoxia-induced pulmonary artery smooth muscle cells by up-regulating A2a receptor via the SDF-1/CXCR4 signaling pathway. [Abstract]

2018 Dec 12;18(1):330. PMID: 30541517
Stem Cells Int

IL-1 β Pretreatment Improves the Efficacy of Mesenchymal Stem Cells on Acute Liver Failure by Enhancing CXCR4 Expression. [Abstract]

2020 Jul 7;2020:1498315. PMID: 32724311
Cell Transplant

Effects of Low-Intensity Pulsed Ultrasound on the Migration and Homing of Human Amnion-Derived Mesenchymal Stem Cells to Ovaries in Rats With Premature Ovarian Insufficiency. [Abstract]

2022 Jan-Dec;31:9636897221129171. PMID: 36282038
Kaohsiung J Med Sci

MiR-32-5p promoted epithelial-to-mesenchymal transition of oral squamous cell carcinoma cells via regulating the KLF2/CXCR4 pathway. [Abstract]

2022 Feb;38(2):120-128. PMID: 34741382
J Diabetes Complications

Plerixafor stimulates adhesive activity and endothelial regeneration of endothelial progenitor cells via elevating CXCR7 expression. [Abstract]

2020 Oct;34(10):107654. PMID: 32741660
Cell Tissue Res

M2 macrophages promote vasculogenesis during retinal neovascularization by regulating bone marrow-derived cells via SDF-1/VEGF. [Abstract]

2020 Jun;380(3):469-486. PMID: 31989253
Brain Behav

Repetitive Transcranial Magnetic Stimulation Improves Cognitive Impairment via the Regulation of White Matter Injury in Rats With Ischemic Stroke. [Abstract]

2025 Dec;15(12):e71117. PMID: 41355332
PLoS One

CXCR4 inhibition with AMD3100 attenuates amphetamine induced locomotor activity in adolescent Long Evans male rats. [Abstract]

2021 Mar 1;16(3):e0247707. PMID: 33647040
J Steroid Biochem Mol Biol

The ERβ-CXCL19/CXCR4-NFκB pathway is critical in mediating the E2-induced inflammation response in the orange-spotted grouper (Epinephelus coioides). [Abstract]

2021 Sep:212:105926. PMID: 34091027
Exp Ther Med

Repetitive transcranial magnetic stimulation increases neurological function and endogenous neural stem cell migration via the SDF-1α/CXCR4 axis after cerebral infarction in rats. [Abstract]

2021 Sep;22(3):1037. PMID: 34373723
Biochem Biophys Res Commun

Assessing the effect and related mechanism of naringenin on the proliferation, osteogenic differentiation and endothelial differentiation of human periodontal ligament stem cells. [Abstract]

2021 Jan 1;534:337-342. PMID: 33250176
Oncol Lett

Targeting CXC motif chemokine receptor 4 inhibits the proliferation, migration and angiogenesis of lung cancer cells. [Abstract]

2018 Sep;16(3):3976-3982. PMID: 30128017
Anticancer Drugs

CXCR4 blockade with AMD3100 enhances Taxol chemotherapy to limit ovarian cancer cell growth. [Abstract]

2017 Oct;28(9):935-942. PMID: 28817386
Cell Physiol Biochem

MicroRNA-381 Favors Repair of Nerve Injury Through Regulation of the SDF-1/CXCR4 Signaling Pathway via LRRC4 in Acute Cerebral Ischemia after Cerebral Lymphatic Blockage. [Abstract]

2018;46(3):890-906. PMID: 29669322

Plerixafor purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;46(3):890-906. [Abstract]

The protein expression of LRRC4, SDF-1, CXCR4, ERK, Slit2 and VEGF in the brain tissue of rats is determined by Western blotting.
bioRxiv

Dietary fructose promotes MASH/HCC progression through enhanced intestinal HIF-2α-dependent iron absorption. [Abstract]

2026 Jun 11:2026.06.07.729655. PMID: 42327230
Res Sq

Cellular context and ligand class shape CXCR4-CCR5 heteromerization in live cells. [Abstract]

2026 May 20:rs.3.rs-9499667. PMID: 42239782
University of Pittsburgh

2026.
Res Sq

2026 Feb 2.
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2026 Mar 23.
bioRxiv

2025 Oct 7.
Res Sq

2025 Aug 07.
Res Sq

2025 Mar 16.
SSRN

2025 Jan 13.
University of Zagreb

2024 May 23.
Research Square Preprint

2023 Oct 23.
Ruprecht-Karls-University Heidelberg

2023 Aug 3.
Research Square Preprint

2022 Jul.
SSRN

5 Feb 2022.
Uppsala University

2022 Feb.
J Oncol

Exosomes Derived from RM-1 Cells Promote the Recruitment of MDSCs into Tumor Microenvironment by Upregulating CXCR4 via TLR2/NF- κ B Pathway. [Abstract]

2021 Oct 8:2021:5584406. PMID: 34659412
Stem Cell Res Ther

Important role of the SDF-1/CXCR4 axis in the homing of systemically transplanted human amnion-derived mesenchymal stem cells (hAD-MSCs) to ovaries in rats with chemotherapy-induced premature ovarian insufficiency (POI). [Abstract]

2022 Feb 23;13(1):79. PMID: 35197118
Oxid Med Cell Longev

Recombinant High-Mobility Group Box 1 (rHMGB1) Promotes NRF2-Independent Mitochondrial Fusion through CXCR4/PSMB5-Mediated Drp1 Degradation in Endothelial Cells. [Abstract]

2021 Aug 2;2021:9993240. PMID: 34394840
Research Square Preprint

2021 Aug.
Universität Hamburg

2021 Mar 19.
Patent

US20200360478A1.
Patent

US20190133998A1.
University of Munich

2019 Apr.
Chinese Journal of Tissue Engineering Research

2014,18(45): 7327-7332.

Solvent & Solubility

In Vitro:

Ethanol : 50 mg/mL (99.45 mM; Need ultrasonic)

DMSO : 1.92 mg/mL (3.82 mM; ultrasonic and warming and adjust pH to 7 with 1 M HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9889 mL

9.9447 mL

19.8894 mL

5 mM

0.3978 mL

1.9889 mL

3.9779 mL

10 mM

0.1989 mL

0.9945 mL

1.9889 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

U87MG cells are seeded in 96-well plates at the density of 6×10³ cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]^[4]

Mice^[3]
Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housing environment, which is SPF and had a temperature of 22°C and a 12h/12h light/dark cycle for a week. Then, they are randomly divided into following experimental groups, with 8 mice in each group: normal (no specific intervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (mice received UUO surgery and the same volume of PBS). AMD3100 and PBS are administered via intraperitoneal injection every day until sacrifice.
Rats^[4]
The CXCR4 antagonist, AMD3100 dissolved in H₂O, is delivered in the type 2 diabetic sand rat model at a dose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD3100 6mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is delivered via minipump for a period of one week.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926. [Content Brief]

[2]. Seki JT, et al. Chemical Stability of Plerixafor after Opening of Single-Use Vial. Can J Hosp Pharm. 2017 Jul-Aug;70(4):270-275. [Content Brief]

[3]. Zabel BA, et al. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol. 2009 Sep 1;183(5):3204-11. [Content Brief]

[4]. De Clercq E, et al. Mozobil® (Plerixafor, AMD3100), 10 years after its approval by the US Food and Drug Administration. Antivir Chem Chemother. 2019 Jan-Dec;27:2040206619829382. [Content Brief]

[5]. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55. [Content Brief]

[6]. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616. [Content Brief]

[7]. Schols D, et al. HIV co-receptor inhibitors as novel class of anti-HIV drugs. Antiviral Res. 2006 Sep;71(2-3):216-26. [Content Brief]

[8]. Zheng J, et al. Toward Normalization of the Tumor Microenvironment for Cancer Therapy. Integr Cancer Ther. 2019;18:1534735419862352. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.9889 mL	9.9447 mL	19.8894 mL	49.7235 mL
Ethanol	5 mM	0.3978 mL	1.9889 mL	3.9779 mL	9.9447 mL
	10 mM	0.1989 mL	0.9945 mL	1.9889 mL	4.9724 mL
	15 mM	0.1326 mL	0.6630 mL	1.3260 mL	3.3149 mL
	20 mM	0.0994 mL	0.4972 mL	0.9945 mL	2.4862 mL
	25 mM	0.0796 mL	0.3978 mL	0.7956 mL	1.9889 mL
	30 mM	0.0663 mL	0.3315 mL	0.6630 mL	1.6575 mL
	40 mM	0.0497 mL	0.2486 mL	0.4972 mL	1.2431 mL
	50 mM	0.0398 mL	0.1989 mL	0.3978 mL	0.9945 mL
	60 mM	0.0331 mL	0.1657 mL	0.3315 mL	0.8287 mL
	80 mM	0.0249 mL	0.1243 mL	0.2486 mL	0.6215 mL

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