Catalog No.S8030 Synonyms: JM 3100
Molecular Weight(MW): 502.78
Plerixafor (AMD3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.
Cited by 23 Publications
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|Description||Plerixafor (AMD3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.|
Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4.  Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. 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 does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. 
|In vivo||A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis.  Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. |
|In vitro||Ethanol||100 mg/mL (198.89 mM)|
|Water||3 mg/mL warmed (5.96 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03653247||Recruiting||Biological: Plerixafor|Drug: Busulfan|Genetic: BIVV003||Sickle Cell Disease||Bioverativ a Sanofi company|Bioverativ Therapeutics Inc.||June 28 2019||Phase 1|Phase 2|
|NCT03547830||Recruiting||Drug: Plerixafor|Drug: Gcsf||Chronic Granulomatous Disease||Federal Research Institute of Pediatric Hematology Oncology and Immunology||April 13 2019||Phase 2|
|NCT03442673||Recruiting||Drug: Vinorelbine|Drug: Gemcitabine|Drug: G-CSF||Multiple Myeloma||University Hospital Inselspital Berne||September 17 2018||Phase 2|
|NCT03226691||Completed||Drug: Plerixafor||Sickle Cell Disease||National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)||July 25 2017||Phase 1|
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Frequently Asked Questions
How about the half-life of the product (Cat S8030)?
The biological half-life for this drug is 3-5 hours: https://en.wikipedia.org/wiki/Plerixafor.