Plerixafor (AMD3100) 8HCl

製品コードS3013 バッチS301303

印刷

化学情報

Chemical Structure Synonyms JM 3100 8HCl,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H54N8.8HCl
分子量 794.47 CAS No. 155148-31-5
Solubility (25°C)* 体外 Water 100 mg/mL (125.87 mM)
DMSO Insoluble
Ethanol 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,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl is the hydrochloride of Plerixafor, 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 can be used as an anti-HIV agent.
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
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 DuraporeTM 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.
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.

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 , , Int J Mol Sci, 2016, 17(6): 943.]

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：

Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Vascular regeneration and skeletal muscle repair induced by long-term exposure to SDF-1α derived from engineered mesenchymal stem cells after hindlimb ischemia [ Exp Mol Med, 2023, 10.1038/s12276-023-01096-9] PubMed: 37779148
PDGF-BB is involved in HIF-1α/CXCR4/CXCR7 axis promoting capillarization of hepatic sinusoidal endothelial cells [ Heliyon, 2023, 9(1):e12715] PubMed: 36685431
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
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
Targeting vasoactive intestinal peptide-mediated signaling enhances response to immune checkpoint therapy in pancreatic ductal adenocarcinoma [ Nat Commun, 2022, 13(1):6418] PubMed: 36302761
Atypical chemokine receptor 3 induces colorectal tumorigenesis in mice by promoting β-arrestin-NOLC1-fibrillarin-dependent rRNA biogenesis [ Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x] PubMed: 35365782
MIF/CXCR4 signaling axis contributes to survival, invasion, and drug resistance of metastatic neuroblastoma cells in the bone marrow microenvironment [ BMC Cancer, 2022, 22(1):669] PubMed: 35715791
CXCR4 antagonist AMD3100 enhances therapeutic efficacy of transcatheter arterial chemoembolization in rats with hepatocellular carcinoma [ Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540] PubMed: 35467082

長期の保管のために-20°Cの下で製品を保ってください。

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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