1. GPCR/G Protein
    Immunology/Inflammation
    Anti-infection
  2. CXCR
    HIV
  3. AMD 3465

AMD 3465 (Synonyms: GENZ-644494)

Cat. No.: HY-15971A
Handling Instructions

AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

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

AMD 3465 Chemical Structure

AMD 3465 Chemical Structure

CAS No. : 185991-24-6

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Top Publications Citing Use of Products

    AMD 3465 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2021 Mar 24;138:111476.

    The results of western blotting showed that high glucose inhibited the activation of the cell cycle pathway, the expression level of CDK4, CDK6, Nusap1, and Cyclin D1 are reduced. However, under the action of AMD3465 (10 μM), the expression level of proteins is significantly higher than that of the HG group.

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    Description

    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

    IC50 & Target[1]

    12G5 mAb-CXCR4

    0.75 nM (IC50, in SupT1 cells)

    CXCL12AF647-CXCR4

    18 nM (IC50, in SupT1 cells)

    X4 HIV-1 (IIIB)

    12.3 nM (IC50, in MT-4 cells)

    X4 HIV-1 (NL4.3)

    6.1 nM (IC50, in MT-4 cells)

    X4 HIV-1 (NL4.3AMD3100)

    2822 nM (IC50, in MT-4 cells)

    X4 HIV-1 (RF)

    7.4 nM (IC50, in MT-4 cells)

    X4 HIV-1 (HE)

    9.8 nM (IC50, in MT-4 cells)

    HIV-2 (ROD)

    12.3 nM (IC50, in MT-4 cells)

    HIV-2 (EHO)

    12.3 nM (IC50, in MT-4 cells)

    In Vitro

    AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells. AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM, but shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78β and MIP-1β in U87.CD4.CCR5 cells. AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses. AMD3465 is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM. The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM[1]. AMD 3465 inhibits CXCL-12-induced growth in U87 and Daoy cells. AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells[2].

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

    In Vivo

    AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts[2].

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

    Molecular Weight

    410.60

    Formula

    C₂₄H₃₈N₆

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Cell Assay
    [2]

    Following serum starvation for 24 h, astrocytes, granule cells, U87 cells, and Daoy cells are treated with 1 μg/mL CXCL12, 2.5 ng/mL AMD 3465, 200 μM rolipram, or 10 μM forskolin. Daoy and U87 cell growth in culture is measured by trypan blue exclusion after 24 and 48 h of treatment, respectively[2].

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

    Animal Administration
    [2]

    Mice[2]
    Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates. Two weeks after tumor cell implantation, cohorts of mice with approximately equivalent tumor bioluminescence are divided into equal control and treatment groups. Animals in AMD 3465 experiments receive s.c. osmotic pumps loaded with 10 mg/mL AMD 3465 in sterile PBS or PBS alone. The infusion rate is 0.25 μL/h (50 μg/d). For the experiments with rolipram or caffeine, mice in the treatment groups receive oral administration of rolipram (5 μg/g/d) or caffeine (100 μg/g/d). The concentration of drug in the water is determined from daily measurements of water consumption by each animal over the course of 7 days. Concentrations are adjusted based on water consumption to provide the prescribed dose[2].

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

    References
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