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Plerixafor

Cat. No. M1898
Plerixafor Structure
Synonym:

AMD3100

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 36  USD40 In stock
10mg USD 63  USD70 In stock
25mg USD 112.5  USD125 In stock
50mg USD 184.5  USD205 In stock
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Quality Control
Biological Activity

Plerixafor is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4. The CXCR4 alpha-chemokine receptor and one of its ligands, SDF-1, are important in hematopoietic stem cell homing to the bone marrow and in hematopoietic stem cell quiescence. CXCR-4 antagonist Plerixafor is one of the most efficient bone marrow stem cell mobilizers. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor results in the rapid and reversible mobilization of hematopoietic stem cells into the peripheral circulation and is synergistic when combined with G-CSF.

Customer Product Validations & Biological Datas
Source Tianjin Med J (2015). Figure 4. AMD3100 (Abmole Bioscience)
Method Caspase-3 Assay
Cell Lines EPCs
Concentrations 25 μmol/L
Incubation Time 24、48、96 h
Results Compared with the control group, GLP-1 overexpression decreased Caspase-3 mRNA expression and Caspase-3 activity, both of which were significantly decreased after 48 h of GLP-1 treatment, and the most significant down-regulation trend was shown at 96 h (P<0.05). When the SDF-1/CXCR4 signaling pathway was blocked, the inhibitory effect of GLP-1 on Caspase-3 mRNA expression and Caspase-3 activity were significantly decreased (P <0.05). As shown in figure 4.
Source Tianjin Med J (2015). Figure 3. AMD3100 (Abmole Bioscience)
Method MTT
Cell Lines EPCs
Concentrations 25 μmol/L
Incubation Time 24、48、96 h
Results Compared with the control group, GLP-1 overexpression significantly promoted cell proliferation (P<0.05). After blocking the SDF-1/CXCR4 signaling pathway with AMD3100 blocker, the proliferation effect of GLP-1 on EPCs was significantly decreased (P<0.05), as shown in Figure 3.
Source Tianjin Med J (2015). Figure 2. AMD3100 (Abmole Bioscience)
Method qPCR
Cell Lines EPCs
Concentrations
Incubation Time 24、48、96 h
Results Compared with the control group, GLP-1 overexpression significantly increased the mRNA expressions of C/EBPα and PPARγ (P<0.05) in a time dependent manner. After the SDF-1/CXCR4 signaling pathway was blocked, GLP-1 significantly inhibited the mRNA expression of C/EBPα and PPARγ (P < 0.05), as shown in Figure 2.
Source Tianjin Med J (2015). Figure 1. AMD3100 (Abmole Bioscience)
Method western blot
Cell Lines EPCs
Concentrations 0、5、15 and 25 μmol/L
Incubation Time 48h
Results Compared with the control group (0.465±0.085), CXCR4 protein expression was significantly decreased after treatment with different doses of AMD3100, and the effect of 25 μmol/L AMD3100 group (0.054±0.023) was the most significant (F=16.347, P < 0.05), see Figure 1. It was proved that 25 μmol/L AMD3100 had the best blocking effect and could be used for subsequent blocking experiments.
Protocol
Cell Experiment
Cell lines OS cell lines (LM8 and Dunn)
Preparation method MTT assay.
The effects of CXCL12 and AMD3100 on the survival of two OS cell lines (LM8 and Dunn) were assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at 2×103/well in DMEM-h. After overnight growth, the cells were cultured for 7 days in FBS-free medium in the presence of 0 or 100 ng/ml CXCL12, 30 μM AMD3100 alone or 100 ng/ml CXCL12 with 10, 20 or 30 μM AMD3100. The FBS-free cells without 100 ng/ml CXCL12 or AMD3100 served as the control group. After the 7 day incubation, 20 μl MTT (5 mg/ml; Sigma, St. Louis, MO, USA) was added into each well and incubated for 4 h at 37°C. Culture medium was removed and 150 μl dimethylsulfoxide was added. The optical density (OD) was then measured using a model ELx800 microplate reader (Bio-Tech instruments inc.) at 490 nm. The cell viability was calculated using the equation: Cell viability (%) = (OD490nm of treatment/OD490nm of control) ×100%.
Concentrations 30 μM
Incubation time 7 days
Animal Experiment
Animal models orthotopic animal model of OS in Ten 4-week-old female C3H mice
Formulation PBS
Dosages 5 mg/kg every 2 days
Administration tail vein injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 502.78
Formula C28H54N8
CAS Number 110078-46-1
Purity 99.24%
Solubility Ethanol 70 mg/mL
Water 2 mg/mL
Storage at -20°C
References

AMD3100 reduces CXCR4-mediated survival and metastasis of osteosarcoma by inhibiting JNK and Akt, but not p38 or Erk1/2, pathways in in vitro and mouse experiments.
Liao YX, et al. Oncol Rep. 2015 Jul;34(1):33-42. PMID: 25997540.

Plerixafor, a CXCR4 antagonist, mitigates skin radiation-induced injury in mice.
Kim JH, et al. Radiat Res. 2012 Sep;178(3):202-6. PMID: 22799631.

Plerixafor, a CXCR4 antagonist for the mobilization of hematopoietic stem cells.
Uy GL, et al. Expert Opin Biol Ther. 2008 Nov;8(11):1797-804. PMID: 18847313.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Plerixafor, AMD3100 supplier, CXCR, inhibitors

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