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MedKoo Cat#: 596233 | Name: Plerixafor free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Plerixafor, also known as AMD3100, is a bicyclam with hematopoietic stem cell-mobilizing activity. In the form of its zinc complex, plerixafor acts as an antagonist (or perhaps more accurately a partial agonist) of the alpha chemokine receptor CXCR4 and an allosteric agonist of CXCR7. 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. Plerixafor has been found to be a strong inducer of mobilization of hematopoietic stem cells from the bone marrow to the bloodstream as peripheral blood stem cells.[10] Additionally, plerixafor inhibits CD20 expression on B cells by interfering with CXCR4/SDF1 axis that regulates its expression.

Chemical Structure

Plerixafor free base
Plerixafor free base
CAS#110078-46-1 (free base)

Theoretical Analysis

MedKoo Cat#: 596233

Name: Plerixafor free base

CAS#: 110078-46-1 (free base)

Chemical Formula: C28H54N8

Exact Mass: 502.4471

Molecular Weight: 502.80

Elemental Analysis: C, 66.89; H, 10.83; N, 22.29

Price and Availability

Size Price Availability Quantity
250mg USD 350.00 2 Weeks
500mg USD 550.00 2 Weeks
1g USD 750.00 2 Weeks
2g USD 1,350.00 2 Weeks
5g USD 2,650.00 2 Weeks
10g USD 4,150.00 2 Weeks
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Related CAS #
155148-31-5 (HCl) 110078-46-1 (free base)
Synonym
Plerixafor; Mozobil; JKL 169; AMD3100; AMD-3100; AMD 3100; JM 3100; JM3100; JM-3100; SDZ-SID-791; JLK-169; SID-791; JM-2987;
IUPAC/Chemical Name
1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene
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
SMILES Code
C1(CN2CCNCCCNCCNCCC2)=CC=C(CN3CCNCCCNCCNCCC3)C=C1
Appearance
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
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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7.
In vitro activity:
AMD3100 has been shown to be a CXCR4 receptor antagonist, and to block HIV infection of T-tropic, X4-using, virus in vitro and in vivo. Using the CCRF-CEM T-cell line that constitutively expresses CXCR4 we confirmed that AMD3100 was an antagonist of SDF-1/CXCL12 ligand binding (IC50=651+/-37 nM). This study has also shown that AMD3100 inhibits SDF-1 mediated GTP-binding (IC50=27+/-2.2 nM), SDF-1 mediated calcium flux (IC50=572+/-190 nM), and SDF-1 stimulated chemotaxis (IC50=51+/-17 nM). Reference: Biochem Pharmacol. 2006 Aug 28;72(5):588-96. https://pubmed.ncbi.nlm.nih.gov/16815309/
In vivo activity:
Full thickness excisional skin wounds were created on the backs of db/db mice, treated with AMD3100 or saline, and examined 0, 7, and 14 days later (Figure 1A). On day 14, the extent of wound closure was significantly greater (P<0.0001) in mice treated with AMD3100 (86.97±2.55%) than in saline-treated mice (33.07±1.82%) (Figure 1B), and histological scores were significantly higher for AMD3100-treated wounds than for wounds treated with saline (Figures 1C-E) (epithelialization: AMD3100, 4.250±0.250, saline, 2.000±0.408, P<0.005; granulation: AMD3100, 4.750±0.479, saline, 2.250±0.479, P<0.01; inflammation: AMD3100, 3.750±0.250, saline, 2.500±0.289; P<0.05) (Figures 1C-E); inflammation scores were also significantly higher for AMD3100-treated wounds on day 7 (AMD3100, 3.500±0.289, saline, 1.500±0.289, P<0.005). Reference: J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20. https://pubmed.ncbi.nlm.nih.gov/22048734/
Solvent mg/mL mM
Solubility
DMF 1.0 1.99
DMSO 1.0 1.99
Ethanol 53.3 106.07
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 502.80 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.

Recalculate based on batch purity %
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. Zhu WB, Zhao ZF, Zhou X. AMD3100 inhibits epithelial-mesenchymal transition, cell invasion, and metastasis in the liver and the lung through blocking the SDF-1α/CXCR4 signaling pathway in prostate cancer. J Cell Physiol. 2019 Jul;234(7):11746-11759. doi: 10.1002/jcp.27831. Epub 2018 Dec 7. PMID: 30537000. 2. Fricker SP, Anastassov V, Cox J, Darkes MC, Grujic O, Idzan SR, Labrecque J, Lau G, Mosi RM, Nelson KL, Qin L, Santucci Z, Wong RS. Characterization of the molecular pharmacology of AMD3100: a specific antagonist of the G-protein coupled chemokine receptor, CXCR4. Biochem Pharmacol. 2006 Aug 28;72(5):588-96. doi: 10.1016/j.bcp.2006.05.010. Epub 2006 Jul 3. PMID: 16815309. 3. Kumar S, Ponnazhagan S. Mobilization of bone marrow mesenchymal stem cells in vivo augments bone healing in a mouse model of segmental bone defect. Bone. 2012 Apr;50(4):1012-8. doi: 10.1016/j.bone.2012.01.027. Epub 2012 Feb 9. PMID: 22342795; PMCID: PMC3339043. 4. Nishimura Y, Ii M, Qin G, Hamada H, Asai J, Takenaka H, Sekiguchi H, Renault MA, Jujo K, Katoh N, Kishimoto S, Ito A, Kamide C, Kenny J, Millay M, Misener S, Thorne T, Losordo DW. CXCR4 antagonist AMD3100 accelerates impaired wound healing in diabetic mice. J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20. doi: 10.1038/jid.2011.356. Epub 2011 Nov 3. PMID: 22048734; PMCID: PMC3276738.
In vitro protocol:
1. Zhu WB, Zhao ZF, Zhou X. AMD3100 inhibits epithelial-mesenchymal transition, cell invasion, and metastasis in the liver and the lung through blocking the SDF-1α/CXCR4 signaling pathway in prostate cancer. J Cell Physiol. 2019 Jul;234(7):11746-11759. doi: 10.1002/jcp.27831. Epub 2018 Dec 7. PMID: 30537000. 2. Fricker SP, Anastassov V, Cox J, Darkes MC, Grujic O, Idzan SR, Labrecque J, Lau G, Mosi RM, Nelson KL, Qin L, Santucci Z, Wong RS. Characterization of the molecular pharmacology of AMD3100: a specific antagonist of the G-protein coupled chemokine receptor, CXCR4. Biochem Pharmacol. 2006 Aug 28;72(5):588-96. doi: 10.1016/j.bcp.2006.05.010. Epub 2006 Jul 3. PMID: 16815309.
In vivo protocol:
1. Kumar S, Ponnazhagan S. Mobilization of bone marrow mesenchymal stem cells in vivo augments bone healing in a mouse model of segmental bone defect. Bone. 2012 Apr;50(4):1012-8. doi: 10.1016/j.bone.2012.01.027. Epub 2012 Feb 9. PMID: 22342795; PMCID: PMC3339043. 2. Nishimura Y, Ii M, Qin G, Hamada H, Asai J, Takenaka H, Sekiguchi H, Renault MA, Jujo K, Katoh N, Kishimoto S, Ito A, Kamide C, Kenny J, Millay M, Misener S, Thorne T, Losordo DW. CXCR4 antagonist AMD3100 accelerates impaired wound healing in diabetic mice. J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20. doi: 10.1038/jid.2011.356. Epub 2011 Nov 3. PMID: 22048734; PMCID: PMC3276738.
1: Jantunen E, Turunen A, Varmavuo V, Partanen A. Impact of plerixafor use in the mobilization of blood grafts for autologous hematopoietic cell transplantation. Transfusion. 2024 Feb 26. doi: 10.1111/trf.17755. Epub ahead of print. PMID: 38407504. 2: Fang Y, Ye PP. [Research Progress on the Application Strategies of Plerixafor in the Peripheral Blood Stem Cell Mobilization for Autologous Transplantation-- Review]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2024 Feb;32(1):322-326. Chinese. doi: 10.19746/j.cnki.issn.1009-2137.2024.01.053. PMID: 38387943. 3: Marcon C, Bertone A, Mauro S, Mestroni R, Battaglia G, Pizzano U, Facchin G, De Martino M, Isola M, Patriarca F, Barillari G, Savignano C. Stem Cells mobilization and collection in allogeneic related and unrelated donors: a single center experience with focus on plerixafor. Transfus Apher Sci. 2023 Dec;62(6):103845. doi: 10.1016/j.transci.2023.103845. Epub 2023 Nov 3. PMID: 37953206. 4: Swinn T, Butler A. Plerixafor use in New Zealand 2016-2019: an observational study. Intern Med J. 2023 Jun;53(6):970-977. doi: 10.1111/imj.15819. Epub 2022 Sep 6. PMID: 35560504. 5: Merati N, Sivachandran S, Jfri A, Ben-Shoshan M, Vinh DC, Popradi G, Litvinov IV. Plerixafor on a WHIM - Promise or Fantasy of a New CXCR4 Inhibitor for This Rare, but Important Syndrome? Skin Therapy Lett. 2022 Mar;27(2):1-5. PMID: 35385630. 6: Romon I, Castillo C, Cid J, Lozano M. Use of plerixafor to mobilize haematopoietic progenitor cells in healthy donors. Vox Sang. 2022 Jan;117(1):6-16. doi: 10.1111/vox.13175. Epub 2021 Jun 23. PMID: 34159611. 7: Bilgin YM. Use of Plerixafor for Stem Cell Mobilization in the Setting of Autologous and Allogeneic Stem Cell Transplantations: An Update. J Blood Med. 2021 Jun 2;12:403-412. doi: 10.2147/JBM.S307520. Erratum in: J Blood Med. 2022 Sep 05;13:483-484. PMID: 34104027; PMCID: PMC8180285. 8: Wang J, Tannous BA, Poznansky MC, Chen H. CXCR4 antagonist AMD3100 (plerixafor): From an impurity to a therapeutic agent. Pharmacol Res. 2020 Sep;159:105010. doi: 10.1016/j.phrs.2020.105010. Epub 2020 Jun 13. PMID: 32544428. 9: Karres D, Ali S, van Hennik PB, Straus S, Josephson F, Thole G, Glerum PJ, Herberts C, Babae N, Herold R, Papadouli I, Pignatti F. EMA Recommendation for the Pediatric Indications of Plerixafor (Mozobil) to Enhance Mobilization of Hematopoietic Stem Cells for Collection and Subsequent Autologous Transplantation in Children with Lymphoma or Malignant Solid Tumors. Oncologist. 2020 Jun;25(6):e976-e981. doi: 10.1634/theoncologist.2019-0898. Epub 2020 Mar 10. PMID: 32154610; PMCID: PMC7288649. 10: Allen ES, Conry-Cantilena C. Mobilization and collection of cells in the hematologic compartment for cellular therapies: Stem cell collection with G-CSF/plerixafor, collecting lymphocytes/monocytes. Semin Hematol. 2019 Oct;56(4):248-256. doi: 10.1053/j.seminhematol.2019.11.003. Epub 2019 Nov 8. PMID: 31836031. 11: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Plerixafor. 2019 Apr 12. PMID: 31643772. 12: De Clercq E. Mozobil® (Plerixafor, AMD3100), 10 years after its approval by the US Food and Drug Administration. Antivir Chem Chemother. 2019 Jan- Dec;27:2040206619829382. doi: 10.1177/2040206619829382. PMID: 30776910; PMCID: PMC6379795. 13: Couban S, Wong PC, Schultz KR. The case for plerixafor to replace filgrastim as the optimal agent to mobilize peripheral blood donors for allogeneic hematopoietic cell transplantation. Exp Hematol. 2019 Feb;70:1-9. doi: 10.1016/j.exphem.2018.11.003. Epub 2018 Nov 11. PMID: 30428338. 14: Douglas KW, Gilleece M, Hayden P, Hunter H, Johnson PRE, Kallmeyer C, Malladi RK, Paneesha S, Pawson R, Quinn M, Raj K, Richardson D, Robinson S, Russell N, Snowden J, Sureda A, Tholouli E, Thomson K, Watts M, Wilson KM. UK consensus statement on the use of plerixafor to facilitate autologous peripheral blood stem cell collection to support high-dose chemoradiotherapy for patients with malignancy. J Clin Apher. 2018 Feb;33(1):46-59. doi: 10.1002/jca.21563. Epub 2017 Jun 20. PMID: 28631842. 15: Plerixafor for Patients Failing Stem Cell Mobilization: A Review of the Clinical and Cost-Effectiveness and Guidelines [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Nov 8. PMID: 28151615. 16: Sancho JM, Duarte R, Medina L, Querol S, Marín P, Sureda A; en representación del Grupo de Trabajo de Movilización de la Sociedad Catalana de Hematología y Hemoterapia y de la Sociedad Catalano-Balear de Transfusión Sanguínea. Movilización de progenitores hematopoyéticos a sangre periférica con plerixafor en pacientes malos movilizadores [Mobilization of peripheral blood stem cells with plerixafor in poor mobilizer patients]. Med Clin (Barc). 2016 Sep 2;147(5):223.e1-223.e7. Spanish. doi: 10.1016/j.medcli.2016.05.019. Epub 2016 Jun 30. PMID: 27374031. 17: Jantunen E, Varmavuo V, Valtola J. Plerixafor injection: a hematopoietic stem cell mobilizer in non-Hodgkin lymphoma and multiple myeloma. Expert Rev Hematol. 2016 Aug;9(8):723-32. doi: 10.1080/17474086.2016.1208082. Epub 2016 Jul 15. PMID: 27355397. 18: Bilgin YM, de Greef GE. Plerixafor for stem cell mobilization: the current status. Curr Opin Hematol. 2016 Jan;23(1):67-71. doi: 10.1097/MOH.0000000000000200. PMID: 26554889. 19: Hartmann T, Hübel K, Monsef I, Engert A, Skoetz N. Additional plerixafor to granulocyte colony-stimulating factors for haematopoietic stem cell mobilisation for autologous transplantation in people with malignant lymphoma or multiple myeloma. Cochrane Database Syst Rev. 2015 Oct 20;2015(10):CD010615. doi: 10.1002/14651858.CD010615.pub2. PMID: 26484982; PMCID: PMC9468901. 20: Goker H, Etgul S, Buyukasik Y. Optimizing mobilization strategies in difficult-to-mobilize patients: The role of plerixafor. Transfus Apher Sci. 2015 Aug;53(1):23-9. doi: 10.1016/j.transci.2015.05.011. Epub 2015 Jun 9. PMID: 26099666.