Plerixafor (AMD 3100)

Alias: JM-3100; AMD3100; AMD 3100; JM-3100; AMD-3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; Plerixafor HCl; MOZOBIL
Cat No.:V1488 Purity: ≥98%
Plerixafor (formerly known as SDZ-SID-791; JLK-169; SID-791;AMD3100, AMD-3100, JM-3100, JM 3100; trade name Mozobil), the so called hematopoeitic stem cell mobilizer,is a novel and potent chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with an IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.
Plerixafor (AMD 3100) Chemical Structure CAS No.: 110078-46-1
Product category: CXCR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Plerixafor (AMD 3100):

  • Plerixafor 8HCl (AMD3100)
  • Plerixafor-d4
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Plerixafor (formerly known as SDZ-SID-791; JLK-169; SID-791; AMD3100, AMD-3100, JM-3100, JM 3100; trade name Mozobil), the so called 'hematopoeitic stem cell mobilizer', is a novel and potent chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with an IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. The bicyclam plerixafor has been approved as an immunostimulant to mobilize hematopoietic stem cells into the bloodstream in cancer patients. It has been shown to have hematopoietic stem cell-mobilizing activity. Plerixafor causes the release of hematopoietic stem cells (HSC) from the bone marrow and their migration into the peripheral circulation by preventing the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Biological Activity I Assay Protocols (From Reference)
Targets
125I-CXCL12-CXCR4 ( IC50 = 44 nM ); 125I-CXCL12-CXCR7; HIV-1 ( EC50 = 1-10 nM ); HIV-2 ( IC50 = 1-10 nM )
ln Vitro

In vitro activity: Plerixafor has a slightly stronger inhibitory potency against CXCL12-mediated chemotaxis than it does against CXCR4.[1]
Plerixafor likewise inhibits the binding of SDF-1/CXCL12 ligand at an IC50 of 651 nM. With IC50 values of 27 nM, 572 nM, and 51 nM, respectively, plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux, and SDF-1 stimulated chemotaxis. Plerixafor neither inhibits receptor binding of LTB4 nor calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5, or CCR7 when stimulated with their cognate ligands. Plerixafor does not cause a calcium flux in CCRF–CEM cells on its own. These cells express several GPCRs, such as CXCR4, CCR4, and CCR7.[2]

ln Vivo
In diabetic mice, a single topical application of Plerixafor increases the production of cytokines, mobilizes bone marrow EPCs, and activates fibroblasts, monocytes/macrophages, and fibroblasts, thereby increasing angiogenesis and vasculogenesis.[3]
Mice are given PBS, IGF1, PDGF, SCF, or VEGF for five days in a row, and Plerixafor on the fifth day. Compared to groups treated with PDGF, SCF, and VEGF in addition to Plerixafor, mice injected with IGF1 plus Plerixafor exhibited the largest colonies in terms of both number and size.[4]
Enzyme Assay
For the competition binding studies against CXCR4, 5 × 105 CCRF-CEM cells and 100 pM 125I-SDF-1α (2200 Ci/mmol) are incubated for three hours at 4 °C in binding buffer (PBS containing 5 mM MgCl2, 1 mM Ca Cl2, 0.25% BSA, pH 7.4) in Milipore DuraporeTM filter plates. After washing with cold 50 mM HEPES and 0.5 M NaCl pH 7.4, unbound 125I-SDF-1α is eliminated. On membranes from CHO-S cells expressing recombinant BLT1, the competition binding assay is carried out. Mechanical cell lysis, high-speed centrifugation, resuspension in 50 mm HEPES buffer containing 5 mM MgCl22, and flash freezing are the steps involved in the preparation of the membranes. The assay mixture comprising 50 mM Tris, pH 7.4, 10 mM MgCl2, 10 mM CaCl2, 4 nM LTB4 combined with 1 nM 3H-LTB4 (195.0 Ci/mmol) and 8 μg membrane is incubated with Plerixafor for one hour at room temperature. Filtration is used to separate the unbound 3H-LTB4 on Millipore Type GF-C filter plates.
Cell Assay
Peptide R, Plerixafor, or CXCL12 are applied to U87MG cells after they are seeded at a density of 6 ×103 cells in 200 μL/well in 96-well plates. During the last two hours of treatment, MTT (5 μg/mL) is added at 24, 48, and 72 hours. Following the removal of the cell medium, 100 μL of DMSO is added, and an LT-4000MS Microplate Reader is used to measure the optical densities at 595 nm. Three separate experiments' worth of measurements are taken in triplicate.
Animal Protocol
Mice: The mice used are male C57bl/6s, aged 6-7 weeks and weighing 20 g. After a week of a 22°C temperature and a 12 hr /12 hr light/dark cycle, the animals are acclimated to their new home in SPF. Next, they are split into three experimental groups at random, each containing eight mice: normal (no special treatment), UUO+AMD3100 (mice that underwent UUO surgery plus 2 mg/kg AMD3100), and UUO+PBS (mice that underwent UUO surgery plus the same amount of PBS). Every day until sacrifice, intraperitoneal injections of AMD3100 and PBS are given.
Rats: The type 2 diabetic sand rat model is used to administer the CXCR4 antagonist AMD3100 dissolved in H2O at a dose of 6 mg/kg per day for eight weeks. The impact of AMD3100 (6 mg/kg/d) CXCR4 antagonism on the quantity of regulatory T cells is investigated in complementary investigations. The AMD3100 or vehicle is supplied via minipump for a week in order to conduct these studies.
References

[1]. J Immunol . 2009 Sep 1;183(5):3204-11.

[2]. Biochem Pharmacol . 2006 Aug 28;72(5):588-96.

[3]. J Invest Dermatol . 2012 Mar;132(3 Pt 1):711-20.

[4]. Bone . 2012 Apr;50(4):1012-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H54N8
Molecular Weight
502.78
Exact Mass
502.45
Elemental Analysis
C, 66.89; H, 10.83; N, 22.29
CAS #
110078-46-1
Appearance
Solid powder
SMILES
C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3
InChi Key
YIQPUIGJQJDJOS-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H54N8/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36/h5-8,29-34H,1-4,9-26H2
Chemical Name
1-[[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methyl]-1,4,8,11-tetrazacyclotetradecane
Synonyms
JM-3100; AMD3100; AMD 3100; JM-3100; AMD-3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; Plerixafor HCl; MOZOBIL
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: ~3 mg/mL (~5.96 mM)
Ethanol: ~100 mg/mL (~198.9 mM)
Solubility (In Vivo)
30%Propylene glycol, 5%Tween 80, 65% D5W: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT06141304 Active
Recruiting
Drug: Plerixafor Relapsed Adult ALL
Relapsed Adult AML
The First Hospital of Jilin
University
September 1, 2023 Phase 2
NCT02193191 Active
Recruiting
Drug: Plerixafor Sickle Cell Disease Memorial Sloan Kettering
Cancer Center
September 2014 Phase 1
NCT03182426 Active
Recruiting
Drug: Plerixafor
Drug: Alemtuzumab
Diabetes Mellitus, Type 1 University of Alberta August 15, 2017 Phase 1
Phase 2
NCT03653247 Active
Recruiting
Biological: Plerixafor
Drug: Busulfan
Sickle Cell Disease Sangamo Therapeutics March 6, 2019 Phase 1
Phase 2
NCT03664830 Recruiting Drug: Plerixafor Sickle Cell Disease City of Hope Medical Center September 19, 2018 Phase 1
Biological Data
  • Plerixafor (AMD3100)

  • Plerixafor (AMD3100)

    Wound-healing in diabetic mice. J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20.
  • Plerixafor (AMD3100)

    J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20.
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