Plerixafor (Synonyms: AMD 3100; JM3100; SID791)

Name: Plerixafor
Brand: MedChemExpress
SKU: HY-10046
Rating: 5.0 (79 reviews)

Cat. No.: HY-10046 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Plerixafor Chemical Structure

CAS No. : 110078-46-1

Size	Price	Stock	Quantity
5 mg	USD 54	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 142	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 199	In-stock	Estimated Time of Arrival: December 31
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Based on 79 publication(s) in Google Scholar

Other Forms of Plerixafor:

67 Publications Citing Use of MCE Plerixafor

RT-PCR

Proliferation Assay

IHC

: 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.

: 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: 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.

: 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.

: 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.

: 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.

: 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).

: 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.

: 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.

: 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.

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HIV HIV-1 HIV-2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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	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	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	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]
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	> 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 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 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 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: 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 human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 26094944]
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	0.008 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	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	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	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	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]
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]

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

Molecular Weight

502.78

Formula

C₂₈H₅₄N₈

CAS No.

110078-46-1

Appearance

Solid

Color

White to off-white

SMILES

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

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

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)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 3 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 3 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (247 KB) HNMR (252 KB) RP-HPLC (206 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]

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

Complete Stock Solution Preparation Table

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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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Plerixafor (Synonyms: AMD 3100; JM3100; SID791)

Customer Review

Other Forms of Plerixafor:

Plerixafor Related Antibodies

67 Publications Citing Use of MCE Plerixafor

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CXCR Isoform Specific Products:

View All HIV Isoform Specific Products:

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