| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Targets |
CXCR4
Peptide R TFA specifically targets the CXCR4 chemokine receptor, a G protein-coupled receptor (GPCR) that plays a critical role in cell migration, proliferation, and survival. The CXCL12/CXCR4 signaling axis is a key driver of tumor cell directional migration and metastasis. As a potent CXCR4 antagonist, Peptide R TFA blocks CXCL12-mediated cell migration, ERK phosphorylation, and CXCR4 internalization. By disrupting the CXCL12/CXCR4 interaction, it effectively targets the tumor stroma and inhibits the metastatic spread of CXCR4-overexpressing tumor cells, including those in leukemia, colon cancer, and melanoma. |
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| ln Vitro |
In vitro, Peptide R TFA acts as a specific CXCR4 antagonist. An analogue of Peptide R (compound 10) inhibits CXCL12-induced cell chemotaxis with an IC₅0 ≤ 100 nM in various cancer cell lines, including Jurkat (leukemia) and HCT116 (colon cancer) cells. It effectively suppresses CXCL12-mediated cell migration, ERK phosphorylation, and CXCR4 internalization. In drug delivery studies, Peptide R TFA-conjugated liposomes (PL-Peptide R-DOX) efficiently delivered doxorubicin to CXCR4-expressing cell lines, resulting in a decreased IC₅0 for doxorubicin and demonstrating targeted drug delivery.
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| ln Vivo |
In vivo, Peptide R TFA has demonstrated significant efficacy in targeting the tumor stroma and inhibiting metastasis. In a B16-CXCR4 melanoma lung metastasis mouse model (C57BL/6 mice), treatment with Peptide R TFA-conjugated doxorubicin liposomes (PL-Peptide R-DOX) resulted in fewer lung metastases compared to PL-DOX-treated mice. The peptide's excellent tumor stroma remodeling ability makes it applicable for research on solid tumors such as glioblastoma. The peptide can be formulated in 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline for in vivo administration.
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| Enzyme Assay |
Not directly applicable; Peptide R TFA is a CXCR4 antagonist, and its binding affinity is typically measured using functional assays rather than simple enzyme/receptor binding assays. For competitive binding studies, the CXCR4 receptor is often expressed on the surface of cells (e.g., Jurkat). A radiolabeled CXCR4 ligand (such as ¹2⁵I-SDF-1 or 3H-labeled AMD3100) is incubated with the cells in the presence of varying concentrations of Peptide R TFA. Bound radioactivity is separated by filtration, and the IC₅0 is calculated. The Ki value can be derived using the Cheng-Prusoff equation. Alternatively, surface plasmon resonance (SPR) can be used to measure direct binding kinetics.
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| Cell Assay |
CXCR4-mediated cell migration (chemotaxis) assays are used to evaluate the functional antagonism of Peptide R TFA. Jurkat or HCT116 cells are loaded into the upper chamber of a transwell plate (pore size 5-8 um) containing a chemoattractant (CXCL12, 10-100 ng/mL) in the lower chamber. Various concentrations of Peptide R TFA (0.1-1000 nM) are added to both chambers. After 2-4 hours of incubation at 37degC, cells that have migrated to the lower chamber are quantified by fluorescence (using Calcein-AM pre-labeled cells) or by manual counting. The IC₅0 for inhibition of chemotaxis is calculated. ERK phosphorylation and CXCR4 internalization can be assessed by Western blot and flow cytometry, respectively.
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| Animal Protocol |
Melanoma lung metastasis mouse model: B16-CXCR4 melanoma cells are injected intravenously (tail vein) into C57BL/6 mice (6-8 weeks old, n=8-10/group). Mice are treated with Peptide R TFA-conjugated liposomal doxorubicin (PL-Peptide R-DOX) or control formulations (e.g., PL-DOX) via intravenous injection. After a defined period (e.g., 14-21 days), mice are sacrificed, and the lungs are harvested. Metastatic nodules on the lung surface are counted. Histological analysis (H&E staining) is performed to confirm tumor cell infiltration. The number of lung metastases is significantly reduced in the PL-Peptide R-DOX group compared to controls, demonstrating effective tumor targeting.
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| ADME/Pharmacokinetics |
Peptide R TFA (MW 900.08 free base) is a cell-permeable peptide. In vivo formulation for animal studies is typically performed using a vehicle of 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline or PBS, resulting in a working solution concentration of up to 2 mg/mL. The pharmacokinetic profile of Peptide R TFA is not extensively documented, but as a cyclic peptide, it exhibits improved plasma stability compared to linear peptides. The disulfide bridge contributes to resistance against proteolytic degradation, potentially extending its half-life in circulation.
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| Toxicity/Toxicokinetics |
Standard safety precautions for research peptides apply. Peptide R TFA is for research use only and is not intended for human consumption. Safety data for Peptide R TFA is not fully detailed; however, as a CXCR4 antagonist, on-target effects may include modulation of the immune system and hematopoiesis. Standard precautions include wearing personal protective equipment (gloves, lab coat, eye protection), working in a fume hood, and avoiding inhalation and skin contact.
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| References |
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| Additional Infomation |
Peptide R TFA is a research-grade CXCR4 antagonist with applications in oncology, particularly for targeting tumor stroma and metastasis in solid tumors like glioblastoma. It is also used in targeted drug delivery systems. It is not an FDA-approved drug. For research use only, not for diagnostic or therapeutic applications. Storage: Powder at -20degC for 3 years; in solvent at -80degC for 1 year.
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| Molecular Formula |
C39H57N13O8S2.XC2HF3O2
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| Molecular Weight |
900.08 (free base)
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| Related CAS # |
Peptide R;1318232-11-9
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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