solo per uso di ricerca
N. Cat.: S3013
Struttura chimica
| Target correlati | Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR |
|---|---|
| Altro CXCR Inibitori | AZD5069 SB 225002 Reparixin (Repertaxin) WZ811 Navarixin (SCH-527123) LIT-927 SX-682 AMG 487 SB 265610 LY2510924 |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dell'attività | PMID |
|---|---|---|---|---|---|---|
| CHOK1 cells | Function assay | Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50=0.81 nM | 17715128 | |||
| GHOST CXCR4 cell line | Function assay | Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line, IC50=0.95 nM | 14698189 | |||
| HEK293 cells | Function assay | 2 days | Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50=2.3 nM | 19451305 | ||
| PBMC cells | Function assay | Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50=3.8 nM | 14698189 | |||
| human MT4 cells | Function assay | 4 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay, EC50=4 nM | 20043638 | ||
| human Jurkat cells | Function assay | Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration, IC50=27.4 nM | 19188071 | |||
| MT-4 cells | Function assay | Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50=65 nM | 14698189 | |||
| rat IR983F cells | Function assay | Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50=108 nM | 19053768 | |||
| CEM-SS cells | Function assay | Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50=127 nM | 14698189 | |||
| human HL60 cells | Function assay | Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50=15.2 μM | 19188071 | |||
| human MOLT4 cells | Function assay | 1000 nM | Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis | 19451305 | ||
| human MT2 cells | Function assay | 1 ug/mL | 4 days | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production at 1 ug/mL after 4 days by ELISA | 21168336 | |
| human U87 cells | Function assay | 1000 nM | Antagonist activity at CXCR4 in human U87 cells assessed as inhibition of SDF1-induced modulation of cAMP production at 1000 nM by TR-FRET assay | 17958344 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B assessed as reduction in cytopathic effect in MT4 cells, EC50=0.011μM | 17034122 | |||
| U87 | Function assay | 15 mins | Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis, IC50=0.695μM | 21105715 | ||
| MT4 | Antiviral assay | Antiviral activity against X4-tropic HIV1 NL4.3 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity, EC50=0.062μM | 22579418 | |||
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days, EC50=0.002μM | 22909088 | ||
| CHO | Function assay | Binding affinity to human recombinant CXCR4 expressed in CHO cells, Kb=0.077μM | 22909088 | |||
| CHO | Function assay | Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis, IC50=0.26μM | 22909088 | |||
| CD44null | Function assay | 7 days | Effect on human GBM2 cell differentiation assessed as increase in CD44null cells after 7 days by flow cytometric analysis | 22909088 | ||
| CD44null | Function assay | 7 days | Effect on human GBM1 cell differentiation assessed as increase in CD44null cells after 7 days by flow cytometric analysis | 22909088 | ||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 794.47 | Formula | C28H54N8.8HCl |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 155148-31-5 | Scarica SDF | Conservazione delle soluzioni stock |
|
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| Sinonimi | JM 3100 8HCl,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride | Smiles | C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl | ||
|
In vitro |
Water : 100 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
|
In vivo |
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Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.
| Targets/IC50/Ki |
CXCL12
(Cell-free assay) 5.7 nM
CXCR4
(Cell-free assay) 44 nM
|
|---|---|
| In vitro |
Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. 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. |
| 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. 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. |
Riferimenti |
|
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Immunofluorescence | CXCR4 β-arrestin2 |
|
28521261 |
(dati da https://clinicaltrials.gov, aggiornato il 2026-09-03)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT06851767 | ENROLLING_BY_INVITATION | X-linked Severe Combined Immunodeficiency; X-SCID; XSCID |
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| NCT06325709 | RECRUITING | Chronic Granulomatous Disease (CGD); X-Linked Chronic Granulomatous Disease |
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| NCT07605416 | RECRUITING | Plasma Cell Leukemia |
National Cancer Institute (NCI) |
2027-04-20 | PHASE2 |
| NCT07775313 | NOT_YET_RECRUITING | WHIM; Warts; Hypogammaglobulinemia; Immunodeficiency; Myelokathexis |
National Institute of Allergy and Infectious Diseases (NIAID) |
2026-09-09 | PHASE1; PHASE2 |
| NCT02015013 | RECRUITING | Idiopathic CD4-Positive; T-Lymphocytopenia |
National Institute of Allergy and Infectious Diseases (NIAID) |
2014-01-15 | PHASE2 |
| NCT06872333 | RECRUITING | Graft Failure; Sickle Cell Disease; Hemoglobinopathies |
Masonic Cancer Center, University of Minnesota |
2024-11-19 | PHASE2 |