WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202260
CAS#: 155148-31-5 (HCl)
Description: Plerixafor, also known as AMD3100, is a bicyclam with hematopoietic stem cell-mobilizing activity. Plerixafor blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). Plerixafor was approved by the U.S. Food and Drug Administration for this indication on December 15, 2008. In Europe, the drug was approved on 29 May 2009.
MedKoo Cat#: 202260
Name: Plerixafor HCl
CAS#: 155148-31-5 (HCl)
Chemical Formula: C28H62Cl8N8
Exact Mass:
Molecular Weight: 794.46
Elemental Analysis: C, 42.33; H, 7.87; Cl, 35.70; N, 14.10
Related CAS #: 155148-31-5 (HCl) 110078-46-1 (free base)
Synonym: AMD3100; AMD-3100; AMD 3100; JM 3100; JM3100; JM-3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; Plerixafor HCl; MOZOBIL.
IUPAC/Chemical Name: 1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene octahydrochloride
InChi Key: UEUPDYPUTTUXLJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H54N8.8ClH/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;8*1H
SMILES Code: [H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.C1(CN2CCNCCCNCCNCCC2)=CC=C(CN3CCNCCCNCCNCCC3)C=C1
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM. |
| In vitro activity: | Plerixafor was investigated for anti-cancer activity in Ewing sarcoma, a rare and aggressive cancer of bone and soft tissues. To investigate plerixafor (AMD3100) as an inhibitor of proliferative CXCR4 signaling in Ewing sarcoma, in vitro cell proliferation and viability assays were performed in several Ewing sarcoma cell lines including the low-passage cell culture DC-ES-6. Unexpectedly, plerixafor induced a dose-dependent increase in relative cell numbers in all cell lines, reaching 1.4 fold at 1 μM in TC-32 and DC-ES6 cells and up to 2.4 fold at 10 μM in VH-64 cells (Fig. 1a). With 72 h of plerixafor treatment, this did not reveal an increase in mitotic cell populations in response to plerixafor. In A673 cells in contrast, plerixafor-directed migration was increased compared to CXCL12, though both did not reach significance. Furthermore, plerixafor appeared to accelerate wound closure in a wound-healing assay (Fig. (Fig.2b).2b). Together these findings indicate an unexpected potential for plerixafor to stimulate proliferation and chemotactic migration of Ewing sarcoma cells in vitro. Cell Commun Signal. 2018; 16: 21. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5960216/ |
| In vivo activity: | To assess the effect of CXCR4 blockade on LPS-mediated injury, male adult C57BL/6 N mice were treated intraperitoneally with LPS, AMD3100, AMD3100 plus LPS, or PBS (control) (n = 7 for all groups except AMD3100 plus LPS, where n = 9). Treatment of the animals with AMD3100 alone led to reduced body temperatures when compared with the control mice. Additionally, AMD3100 alone was able to cause neutrophilia, when compared to the PBS treatment control (Fig. 2a-e) AMD3100 alone also caused a distinct decrease in HO-1 expression in comparison to both LPS-treated and control animals, and after co-administration of AMD3100 and LPS, HO-1 expression was almost completely abolished. AMD3100 appeared to cause a preferential release of neutrophils from the lungs, while inhibiting their return to the bone marrow for elimination from the blood, indicating that CXCR4 blockade can negatively influence physiological defense mechanisms. J Biomed Sci. 2016; 23: 68. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5048674/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| H2O | 70.0 | 88.1 |
The following data is based on the product molecular weight 794.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Liu JM, Zhao K, Du LX, Zhou Y, Long XH, Chen XY, Liu ZL. AMD3100 inhibits the migration and differentiation of neural stem cells after spinal cord injury. Sci Rep. 2017 Mar 6;7(1):64. doi: 10.1038/s41598-017-00141-8. PMID: 28246405; PMCID: PMC5427924. 2. Reeves PM, Abbaslou MA, Kools FRW, Poznansky MC. CXCR4 blockade with AMD3100 enhances Taxol chemotherapy to limit ovarian cancer cell growth. Anticancer Drugs. 2017 Oct;28(9):935-942. doi: 10.1097/CAD.0000000000000518. PMID: 28817386. 3. Xu H, Zhu Z, Huang Y, Ildstad ST. FL/GCSF/AMD3100-mobilized Hematopoietic Stem Cells Induce Mixed Chimerism With Nonmyeloablative Conditioning and Transplantation Tolerance. Transplantation. 2019 Jul;103(7):1360-1371. doi: 10.1097/TP.0000000000002657. PMID: 30747856. 4. Li Z, Zhao R, Fang X, Zhou J, Jiang G, Huang Q, Liu J. AMD3100 Accelerates Reendothelialization of Neointima in Rabbit Saccular Aneurysm After Flow Diverter Treatment. World Neurosurg. 2017 Nov;107:416-423. doi: 10.1016/j.wneu.2017.07.128. Epub 2017 Jul 29. PMID: 28765024. |
| In vitro protocol: | 1. Liu JM, Zhao K, Du LX, Zhou Y, Long XH, Chen XY, Liu ZL. AMD3100 inhibits the migration and differentiation of neural stem cells after spinal cord injury. Sci Rep. 2017 Mar 6;7(1):64. doi: 10.1038/s41598-017-00141-8. PMID: 28246405; PMCID: PMC5427924. 2. Reeves PM, Abbaslou MA, Kools FRW, Poznansky MC. CXCR4 blockade with AMD3100 enhances Taxol chemotherapy to limit ovarian cancer cell growth. Anticancer Drugs. 2017 Oct;28(9):935-942. doi: 10.1097/CAD.0000000000000518. PMID: 28817386. |
| In vivo protocol: | 1. Xu H, Zhu Z, Huang Y, Ildstad ST. FL/GCSF/AMD3100-mobilized Hematopoietic Stem Cells Induce Mixed Chimerism With Nonmyeloablative Conditioning and Transplantation Tolerance. Transplantation. 2019 Jul;103(7):1360-1371. doi: 10.1097/TP.0000000000002657. PMID: 30747856. 2. Li Z, Zhao R, Fang X, Zhou J, Jiang G, Huang Q, Liu J. AMD3100 Accelerates Reendothelialization of Neointima in Rabbit Saccular Aneurysm After Flow Diverter Treatment. World Neurosurg. 2017 Nov;107:416-423. doi: 10.1016/j.wneu.2017.07.128. Epub 2017 Jul 29. PMID: 28765024. |
1: Fricker SP. Physiology and Pharmacology of Plerixafor. Transfus Med Hemother. 2013 Aug;40(4):237-245. Epub 2013 Jul 19. Review. PubMed PMID: 24179472; PubMed Central PMCID: PMC3776399.
2: Pierelli L, Perseghin P. Plerixafor (Mozobil) and other mobilizing agents. Transfus Apher Sci. 2013 Apr;48(2):133-5. doi: 10.1016/j.transci.2013.02.005. Epub 2013 Apr 9. Review. PubMed PMID: 23582743.
3: Tanhehco YC, Vogl DT, Stadtmauer EA, O'Doherty U. The evolving role of plerixafor in hematopoietic progenitor cell mobilization. Transfusion. 2013 Oct;53(10):2314-26. doi: 10.1111/trf.12102. Epub 2013 Jan 30. Review. PubMed PMID: 23362980.
4: Gardellini A, Babic A, Gigli F, Liptrott SJ, Martinelli G, Laszlo D. Successful mobilisation of peripheral blood stem cells in children using plerixafor: a case report and review of the literature. Blood Transfus. 2013 Apr;11(2):308-10. doi: 10.2450/2012.0052-12. Epub 2012 Oct 10. Review. PubMed PMID: 23114521; PubMed Central PMCID: PMC3626485.
5: Dunn D, Vikas P, Jagasia M, Savani BN. Plerixafor in AL amyloidosis: improved graft composition and faster lymphocyte recovery after auto-SCT in patient with end-stage renal-disease. Bone Marrow Transplant. 2012 Aug;47(8):1136-7. doi: 10.1038/bmt.2011.226. Epub 2011 Nov 14. Review. PubMed PMID: 22080973.
6: Jantunen E, Lemoli RM. Preemptive use of plerixafor in difficult-to-mobilize patients: an emerging concept. Transfusion. 2012 Apr;52(4):906-14. doi: 10.1111/j.1537-2995.2011.03349.x. Epub 2011 Oct 7. Review. PubMed PMID: 21981351.
7: Keating GM. Plerixafor: a review of its use in stem-cell mobilization in patients with lymphoma or multiple myeloma. Drugs. 2011 Aug 20;71(12):1623-47. doi: 10.2165/11206040-000000000-00000. Review. PubMed PMID: 21861545.
8: Jantunen E. Novel strategies for blood stem cell mobilization: special focus on plerixafor. Expert Opin Biol Ther. 2011 Sep;11(9):1241-8. doi: 10.1517/14712598.2011.601737. Review. PubMed PMID: 21806478.
9: Mohty M, Duarte RF, Croockewit S, Hübel K, Kvalheim G, Russell N. The role of plerixafor in optimizing peripheral blood stem cell mobilization for autologous stem cell transplantation. Leukemia. 2011 Jan;25(1):1-6. doi: 10.1038/leu.2010.224. Review. PubMed PMID: 21224858.
10: Pelus LM, Farag SS. Increased mobilization and yield of stem cells using plerixafor in combination with granulocyte-colony stimulating factor for the treatment of non-Hodgkin's lymphoma and multiple myeloma. Stem Cells Cloning. 2011 Feb 27;4:11-22. doi: 10.2147/SCCAA.S6713. Review. PubMed PMID: 24198526; PubMed Central PMCID: PMC3781755.
Related CAS#
155148-31-5 ( Plerixafor HCl);
110078-46-1 ( Plerixafor Free base)
