Peptide R
Based on 1 Customer Validation
Peptide R is a cyclic peptide and a specific CXCR4 antagonist. Peptide R exhibits excellent ability to effectively remodel tumor stroma. Peptide R has potential for use in tumor research.
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- CAS No.: 1318232-11-9
- 화학식: C39H57N13O8S2
- 분자량:900.08
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보관:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
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CXCR4 |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | IC50 |
5.2 μM
Compound: 2
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Inhibition of 12G5 anti-CXCR4 antibody binding to CXCR4 in human HT29 cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis
Inhibition of 12G5 anti-CXCR4 antibody binding to CXCR4 in human HT29 cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis
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[PMID: 27571038] |
Peptide R (10 μM; 48-72 h) stably reduces CXCR4 membrane and total CXCR4 protein expression in human glioblastoma U87MG cells over 48 to 72 h of treatment[2].
Peptide R (10 μM; 72 h) reduces proliferation of human glioblastoma U87MG cells by 35% relative to CXCL12-stimulated cells after 72 h of treatment[2].
Peptide R (10 μM; 72 h) significantly reduces the metabolic viability of human glioblastoma U87MG cells after 72 h of treatment[2].
Peptide R (10 μM; 20 h) significantly reduces CXCL12-induced migration of human glioblastoma U87MG cells in a 20 h Transwell assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human glioblastoma U87MG cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Reduced cell number by 35% compared to CXCL12-stimulated cells at 72 h.
Reduced cell number by 20% compared to unstimulated cells at 72 h.
Showed no significant effects at 24 or 48 h.
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Cell Line:human glioblastoma U87MG cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Caused a significant reduction in metabolic activity of U87MG cells at 72 h.
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Cell Line:human glioblastoma U87MG cells
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Concentration:10 μM
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Incubation Time:20 h
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Result:Significantly reduced the percentage of area occupied by migrating U87MG cells.
Hampered cell migration through membrane pores, with very few cells visible on the lower side of the filter compared to CXCL12-stimulated cells.
Peptide R (2 mg/kg; i.p.; twice per day; 23 days) reduces tumor cellularity and abrogates distant glioblastoma cell dissemination, promotes M1 polarization of GAMs, and impairs intra-tumor vasculature in orthotopic U87MG xenografts in CD1 nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 nude mice (6-week-old)[2]
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Dosage:2 mg/kg
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Administration:i.p.; twice per day; 23 days (starting on cell implantation day)
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Result:Reduced tumor cellularity via decreased vimentin expression.
Abrogated dissemination of glioblastoma cells to distant cerebral sites, with no vimentin-positive cells detected in the contralateral hemisphere.
Decreased accumulation of CD11b+ and CD68+ glioma-associated microglia/macrophages (GAMs) at the tumor edge, with mean CD11b fluorescence reduced by ~55% and mean CD68 fluorescence reduced by ~50% compared to vehicle-treated mice.
Promoted M1 pro-inflammatory features in GAMs, with a significant increase in mean inducible nitric oxide synthase (iNOS) fluorescence in the tumor core compared to vehicle-treated mice, and a 2-fold increase in the percentage of CD11b-iNOS colocalized area.
Induced stronger astrogliosis (glial fibrillary acidic protein expression) in tumor tissue.
Chemical Information
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CAS No. 1318232-11-9
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Appearance Solid
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분자량 900.08
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화학식 C39H57N13O8S2
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Color White to off-white
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Sequence
Arg-Ala-Cys-Arg-Phe-Phe-Cys (disulfide bridge:Cys3-Cys7)
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Sequence Shortening
RACRFFC (disulfide bridge:Cys3-Cys7)
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
순도&문서
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Data Sheet (267 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Le Joncour V, et al. Seek & Destroy, use of targeting peptides for cancer detection and drug delivery. Bioorg Med Chem. 2018;26(10):2797-2806. [Content Brief]
[2]. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016;35:55. Published 2016 Mar 25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Peptide R Related Classifications
HY-P4111 Related Classifications
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