1. GPCR/G Protein Immunology/Inflammation Anti-infection
  2. CXCR HIV
  3. Plerixafor

Plerixafor  (Synonyms: AMD 3100; JM3100; SID791)

Cat. No.: HY-10046 Purity: 98.61%
COA Handling Instructions

Plerixafor (AMD 3100) est un antagoniste sélectif de CXCR4 avec un IC50 de 44 nM. Plerixafor, un immunostimulant et un mobilisateur de cellules souches hématopoïétiques (CSH), est un agoniste allostérique du CXCR7. Plerixafor inhibe la réplication de VIH-1 et de VIH-2 avec une EC50 de 1-10 nM.

Plerixafor (AMD 3100) ist ein selektiver CXCR4-Antagonist mit einer IC50 von 44 nM. Plerixafor, ein Immunstimulans und ein Mobilisator für hematopoietic stem cell (HSC), ist ein allosterischer Agonist von CXCR7. Plerixafor hemmt die HIV-1- und HIV-2-Replikation mit einem EC50-Wert von 1-10 nM.

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

Plerixafor Chemical Structure

CAS No. : 110078-46-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in Ethanol USD 92 In-stock
Solid
5 mg USD 54 In-stock
10 mg USD 84 In-stock
50 mg USD 219 In-stock
100 mg USD 417 In-stock
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Customer Review

Based on 71 publication(s) in Google Scholar

Other Forms of Plerixafor:

Top Publications Citing Use of Products

59 Publications Citing Use of MCE Plerixafor

RT-PCR
WB
IF
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]

    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: 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: 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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    Description

    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[1][2][3][4][7].

    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)

    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.
    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 : 1.96 mg/mL (3.90 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

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

      Solubility: ≥ 3 mg/mL (5.97 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 98.61%

    References
    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
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    Plerixafor Related Classifications

    Help & FAQs
    • 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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