Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
Other Sizes |
|
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. 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.
Targets |
125I-CXCL12-CXCR4 ( IC50 = 44 nM ); 125I-CXCL12-CXCR7; HIV-1 ( EC50 = 1-10 nM ); HIV-2 ( IC50 = 1-10 nM )
|
|
---|---|---|
ln Vitro |
|
|
ln Vivo |
|
|
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 |
|
|
References |
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 |
|
|
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 (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
|
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.
Calculation results
Working concentration: mg/mL;
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.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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 |
th> |
---|