Plerixafor (AMD3100)

製品コードS8030 バッチS803001

化学情報

	Synonyms	JM 3100, SID791	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₈H₅₄N₈
	分子量	502.78	CAS No.	110078-46-1
Solubility (25°C)*	体外	Ethanol	100 mg/mL (198.89 mM)
		Water	15 mg/mL warmed with 50ºC water bath (29.83 mM)
		DMSO	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.
in vitro	Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. ^[1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. ^[2]
in vivo	A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. ^[3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. ^[4]

製品説明

Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

in vitro

Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. ^[1]

Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. ^[2]

in vivo

A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. ^[3]

Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. ^[4]

プロトコル(参考用のみ)

キナーゼアッセイ	Receptor binding assays
キナーゼアッセイ	For the competition binding studies against CXCR4, a concentration range of Plerixafor is incubated for 3 hours at 4 °C in binding buffer (PBS containing 5 mM MgCl₂, 1 mM Ca Cl₂, 0.25% BSA, pH 7.4) with 5 × 10⁵ CCRF–CEM cells and 100 pM ¹²⁵I-SDF-1α (2200 Ci/mmol) in Milipore Durapore^TM filter plates. Unbound ¹²⁵I-SDF-1α is removed by washing with cold 50 mM HEPES, 0.5 M NaCl pH 7.4. The competition binding assay against BLT1 is performed on membranes from CHO-S cells expressing recombinant BLT1. The membranes are prepared by mechanical cell lysis followed by high speed centrifugation, re-suspended in 50 mm HEPES, 5 mM MgCl₂ buffer and flash frozen. The membrane preparation is incubated with Plerixafor for 1 hour at room temperature in an assay mixture containing 50 mM Tris, pH 7.4, 10 mM MgCl₂, 10 mM CaCl₂, 4 nM LTB₄ mixed with 1 nM ³H-LTB₄ (195.0 Ci/mmol) and 8 μg membrane. The unbound ³H-LTB₄ is separated by filtration on Millipore Type GF-C filter plates.
細胞アッセイ	細胞株	Cell-free assays
	濃度	44 and 5.7 nM for CXCR4 and CXCL12
	反応時間
	実験の流れ
動物実験	動物モデル	Twelve-week-old C57BL/6 mice with segmental bone defect
	投薬量	5 mg/kg
	投与方法	Administered via i.p.

参考

[4] Kumar S, et al. Bone. 2012, 50(4), 1012-1018.

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カスタマーフィードバック

: Data from [Data independently produced by Blood, 2014, 123(21), 3296-304]

: Data from [Data independently produced by , , J Clin Invest, 2015, 125(8): 3226-40]

: Data from [Data independently produced by , , Angiogenesis, 2016, 19(3):359-71]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The CARD8 inflammasome dictates HIV/SIV pathogenesis and disease progression [ Cell, 2024, 187(5):1223-1237.e16]	PubMed: 38428396
Tumor-associated macrophages promoting PD-L1 expression in infiltrating B cells through the CXCL12/CXCR4 axis in human hepatocellular carcinoma [ Am J Cancer Res, 2024, 14(2):832-853]	PubMed: 38455420
Meningeal macrophages inhibit chemokine signaling in pre-tumor cells to suppress mouse medulloblastoma initiation [ Dev Cell, 2023, 58(20):2015-2031.e8]	PubMed: 37774709
Targeting CXCR4 abrogates resistance to trastuzumab by blocking cell cycle progression and synergizes with docetaxel in breast cancer treatment [ Breast Cancer Res, 2023, 25(1):62]	PubMed: 37280713
A combination therapy of bortezomib, CXCR4 inhibitor, and checkpoint inhibitor is effective in cholangiocarcinoma in vivo [ iScience, 2023, 26(3):106095]	PubMed: 36843847
Cancer-associated fibroblasts induce sorafenib resistance of hepatocellular carcinoma cells through CXCL12/FOLR1 [ BMC Cancer, 2023, 23(1):1198]	PubMed: 38057830
Revealing viral and cellular dynamics of HIV-1 at the single-cell level during early treatment periods [ Cell Rep Methods, 2023, 3(6):100485]	PubMed: 37426753
Adrenal extramedullary hematopoiesis as an inducible model of the adult hematopoietic niche [ bioRxiv, 2023, 10.1101/2023.03.15.531679]	PubMed: None
The CARD8 inflammasome drives CD4+ T-cell depletion in HIV-1 infection [ bioRxiv, 2023, 10.1101/2023.03.18.533283]	PubMed: None
Targeting CXCR4 abrogates resistance to trastuzumab by blocking cell cycle progression and synergizes with docetaxel in breast cancer treatment [ Res Sq, 2023, rs.3.rs-2388864]	PubMed: 36824840

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人間や獣医の診断であるか治療的な使用のためにでない。

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