Plerixafor Chemical Properties

Melting point:

100-102°C

storage temp. 

Hygroscopic, Refrigerator, Under Inert Atmosphere

solubility 

DMSO (Slightly, Heated, Sonicated), Methanol (Slightly), Water (Slightly)

form 

Solid

color 

White to Light Yellow

Stability:

Very Hygroscopic

Plerixafor Usage And Synthesis

Description

Plerixafor-d₄ is intended for use as an internal standard for the quantification of plerixafor by GC- or LC-MS. Plerixafor is a partial antagonist of chemokine receptor 4 (CXCR4) with IC₅₀ values ranging from 0.02 to 0.13 μg/ml for inhibiting calcium flux in peripheral blood mononuclear cells (PBMCs), various types of T cells, and mouse lymphocytic leukemia cells. It is selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC₅₀s = >25 μg/ml). Plerixafor decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(III_B) (EC₅₀ = ~0.02 μg/ml). It rapidly mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation alone and, with a synergistic effect, when used in combination with G-CSF. Plerixafor also increases T cell trafficking in mouse blood, spleen, and central nervous system. Plerixafor (1.25 mg/kg twice per day) decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis.

Chemical Properties

Off-White Solid

Uses

Labelled Plerixafor, it is a hematopoietic stem cell (HSC) mobilizer that inhibits the CXCR4 chemokine receptor and blocks binding of its ligand, stromal cell-derived factor-1-α (SDF-1-α). This agent was approved on Dec. 15, 2008, as treatment in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize HSCs to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin''s lymphoma (NHL) and multiple myeloma (MM).

References

[1] SIGRID HATSE. Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4[J]. FEBS Letters, 2002, 527 1-3: 255-262. DOI: 10.1016/s0014-5793(02)03143-5
[2] E DE CLERCQ. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100.[J]. Antimicrobial Agents and Chemotherapy, 1994, 38 4: 668-674. DOI: 10.1128/aac.38.4.668
[3] DAVID A. HESS . Human Progenitor Cells Rapidly Mobilized by AMD3100 Repopulate NOD/SCID Mice with Increased Frequency in Comparison to Cells from the Same Donor Mobilized by Granulocyte Colony Stimulating Factor[J]. Biology of Blood and Marrow Transplantation, 2007, 13 4: Pages 398-411. DOI: 10.1016/j.bbmt.2006.12.445
[4] GIOVANNI BERNARDINI. CCL3 and CXCL12 regulate trafficking of mouse bone marrow NK cell subsets.[J]. Blood, 2008, 111 7: 3626-3634. DOI: 10.1182/blood-2007-08-106203
[5] ERIN E MCCANDLESS. CXCR4 antagonism increases T cell trafficking in the central nervous system and improves survival from West Nile virus encephalitis.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2008, 105 32: 11270-11275. DOI: 10.1073/pnas.0800898105
[6] MATTHEW C P SMITH. CXCR4 regulates growth of both primary and metastatic breast cancer.[J]. Cancer research, 2004, 64 23: 8604-8612. DOI: 10.1158/0008-5472.can-04-1844

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