pH-Low Insertion Peptide TFA
Based on 1 Customer Validation
pH-Low Insertion Peptide TFA (pHLIP TFA) is a short, pH-responsive peptide capable of inserting across a cell membrane to form a transmembrane helix at acidic pH. pH-Low Insertion Peptide TFA targets the acidic tumor microenvironment for tumors at early and metastatic stages with high specificity, used as a specific ligand. pH-Low Insertion Peptide TFA successfully modifys polylysine polymers to have the pH-responsive capability. pH-Low Insertion Peptide TFA -based targeting of cancer presents an opportunity to monitor metabolic changes and to selectively deliver imaging and therapeutic agents to tumors.
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- Pureza : 95.17%
- Fòrmula: C189H282N42O55S.xC2HF3O2
- Peso molecular:4054.57 (free base)
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Almacenamiento:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Actividad biológica
Descripciòn
In Vitro
pH-Low Insertion Peptide TFA (5 μM, 2 h) combined with peptide nucleic acid (peptide nucleic acid, PNA) significantly increases PNA delivery at pH 6.2 in A549 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A549 cells
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Concentration:5 μM
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Incubation Time:2 h
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Result:Significantly increases PNA delivery combined with PNA at pH 6.2 in A549 cells.
In Vivo
pH-Low Insertion Peptide TFA (10 μM, i.v., a single dose for 24 h) can clearly differentiate between regions of primarily tumor cells and nonmalignant stromal tissues, also accumulates the hypoxia marker Pimonidazole (HY-105129A) and relates to the production of acidic glucose metabolites in MMTV-Py MT mice[2].
pH-Low Insertion Peptide TFA (0.2 μmol/kg, i.v., a single dose for 24 h) demonstrats excellent tumor targeting combined with PNA in mice seeded melanoma tumors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine 4T1 xenograft model[2]
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Dosage:50 μM
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Administration:a single tail vein injection, tumors collected at 4, 24, and 48 h after administration
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Result:The spatial distribution and the intensity profiles of all pHLIP TFAs in tumors were identical in murine 4T1 xenograft mode.
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Animal Model:FVB/N-Tg(MMTV-PyVT)634Mul/J transgenic female mice developed palpable mammary tumors at 12-15 weeks of age[2]
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Dosage:10 μM
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Administration:i.v., a single dose for 24 h
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Result:Clearly differentiated between regions of primarily tumor cells and nonmalignant stromal tissues.
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Animal Model:6-week old C57BL/6 mice seeded melanoma tumors[3]
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Dosage:0.2 μmol/kg
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Administration:intravenously injected via the retro-orbital sinus, a single dose for 24 h
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Result:All the pH-Low Insertion Peptide TFA-PNAs demonstrated excellent tumor targeting.
Chemical Information
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Appearance Solid
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Peso molecular 4054.57 (free base)
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Fòrmula C189H282N42O55S.xC2HF3O2
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Color White to off-white
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Synonyms
pHLIP TFA
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Sequence
Ala-Cys-Glu-Gln-Asn-Pro-Ile-Tyr-Trp-Ala-Arg-Tyr-Ala-Asp-Trp-Leu-Phe-Thr-Thr-Pro-Leu-Leu-Leu-Leu-Asp-Leu-Ala-Leu-Leu-Val-Asp-Ala-Asp-Glu-Thr
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Sequence Shortening
ACEQNPIYWARYADWLFTTPLLLLDLALLVDADET
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Protocolo
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Multiplex immunofluorescence IHC
Multiplex immunofluorescence IHC detects multiple protein biomarkers in one tissue section by sequential antibody staining, HRP-mediated tyramide fluorophore deposition, heat-mediated antibody stripping, nuclear counterstaining, multispectral imaging, spectral unmixing, and digital cell phenotyping; TSA deposits fluorophore near the antigen so the fluorescence signal remains after primary and secondary antibodies are removed, enabling repeated staining cycles, including with antibodies from the same host species. Classic FFPE tumor immune-profiling applications use panels such as CD3, CD8, CD68/CD163, FOXP3, PD-1, PD-L1, pancytokeratin, Ki67, and DAPI to identify tumor cells, immune-cell subsets, checkpoint-marker expression, co-expression phenotypes, cell density, and spatial relationships in the tumor microenvironment.
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Multiplex immunohistochemistry
Multiplex immunohistochemistry (mIHC), also known as tyramide dignal amplification (TSA), is an enzymatic detection method that uses horseradish peroxidase (HRP) to perform high-density in-situ labeling of target proteins or nucleic acids.
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yushuang Wei, et al. pH-responsive pHLIP (pH low insertion peptide) nanoclusters of superparamagnetic iron oxide nanoparticles as a tumor-selective MRI contrast agent. Acta Biomater. 2017 Jun;55:194-203. [Content Brief]
[2]. Adochite RC, et al. Targeting breast tumors with pH (low) insertion peptides[J]. Mol Pharm. 2014 Aug 4;11(8):2896-905. [Content Brief]
[3]. Svoronos AA, et al. Tumor-Targeted, Cytoplasmic Delivery of Large, Polar Molecules Using a pH-Low Insertion Peptide TFA [J]. Mol Pharm. 2020 Feb 3;17(2):461-471. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)