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Plerixafor

Cat. No. M1898
Plerixafor Structure
Synonym:

AMD3100

Size Price Availability Quantity
10mg USD 70 In stock
25mg USD 120 In stock
50mg USD 200 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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 502.78
Formula C28H54N8
CAS Number 110078-46-1
Purity >99%
Solubility Ethanol
Storage at -20°C
Customer Product Validations & Biological Datas
Source 天津医药 (2015). Figure 4. AMD3100 (Abmole Bioscience)
Method Caspase-3 活性检测
Cell Lines EPCs
Concentrations 25 μmol/L
Incubation Time 24、48、96 h
Results 与对照组相比,GLP-1 过表达降低了Caspase-3 mRNA 表达和Caspase-3 活性,其均在GLP-1 作用48 h 后明显降低,96 h 时细胞表现出的下调趋势最为显著(P<0.05)。当SDF-1/CXCR4 信号通路被阻断后,GLP-1 对Caspase-3 mRNA 表达和Caspase-3 活性的抑制作用均明显减弱(P <0.05)。见图4。
Rating
Source 天津医药 (2015). Figure 3. AMD3100 (Abmole Bioscience)
Method MTT 比色法
Cell Lines EPCs
Concentrations 25 μmol/L
Incubation Time 24、48、96 h
Results 与对照组相比,GLP-1 过表达则明显促进了细胞增殖(P<0.05)。AMD3100 阻断剂阻断SDF-1/CXCR4 信 号通路后,GLP-1 对EPCs 的增殖作用明显降低(P<0.05),见图3。
Rating
Source 天津医药 (2015). Figure 2. AMD3100 (Abmole Bioscience)
Method qPCR
Cell Lines EPCs
Concentrations
Incubation Time 24、48、96 h
Results 与对照组相比,GLP-1 过表达显著提高了C/EBPα及PPARγ mRNA 表达(P<0.05),且具时间依赖性。 SDF-1/CXCR4 信号通路被阻断后,GLP-1 对C/EBPα及PPARγ mRNA 表达均明显抑制(P < 0.05),图2。
Rating
Source 天津医药 (2015). Figure 1. AMD3100 (Abmole Bioscience)
Method western blot
Cell Lines EPCs
Concentrations 0、5、15 与25 μmol/L
Incubation Time 48h
Results 与对照组(0.465±0.085)相比,不同剂量AMD3100 作用后,CXCR4 蛋白表达明显降低,25 μmol/L AMD3100 组(0.054±0.023)作用最为明显(F=16.347, P < 0.05),见图1。证明25 μmol/L AMD3100 阻断效果最佳,可用于后续阻断实验。
Rating
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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