| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
WNT5A[1]
Foxy-5 targets WNT5A, a non-canonical member of the Wnt family of secreted glycoproteins. As a WNT5A agonist, Foxy-5 binds to and activates WNT5A receptors (primarily Frizzled-2 and ROR1/ROR2). This activation triggers calcium signaling cascades without affecting the canonical beta-catenin pathway. The compound reduces the metastatic spread of cancer cells with low WNT5A expression. |
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| ln Vitro |
In vitro, Foxy-5 TFA (100 uM, 24 h) inhibits the invasion of DU145 prostate cancer cells by approximately 40%. It triggers cytosolic free calcium signaling without affecting beta-catenin activation and impairs the migration and invasion of epithelial cancer cells. Foxy-5 reduces the number of colon cancer stem cells and inhibits breast cancer cell motility. The peptide lacks a heparan sulfate-binding domain compared to full-length WNT5A.
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| ln Vivo |
In an orthotopic mouse model, Foxy-5 efficiently inhibits the metastatic spread of WNT5A-low prostate cancer cells[1]. In a xenograft mouse model of human colon cancer, Foxy-5 decreases the quantity of colonic cancer stem cells[2].
In vivo, Foxy-5 TFA (2 mg/kg, intraperitoneal injection once daily for 3-9 weeks) significantly reduces the early metastasis and spread of WNT5A-low DU145 prostate cancer cells in an orthotopic mouse model. In a xenograft mouse model of human colon cancer, Foxy-5 (2 mg/kg, i.p. 9 times a day for 7-23 days) reduces the expression of ALDH, DCLK1, and COX-2 while increasing 15-PGDH expression, indicating reduced cancer stem cell numbers. Foxy-5 inhibits breast cancer metastasis in vivo by targeting cell motility. |
| Enzyme Assay |
WNT5A receptor binding assays are typically performed on cell surfaces rather than cell-free. For cell-based receptor binding, culture cancer cells (e.g., DU145, PC3, or MDA-MB-231) expressing WNT5A receptors. Treat cells with increasing concentrations of Foxy-5 (0.1 nM-10 uM) for 30-60 minutes. For competitive binding, co-incubate with fluorescently labeled WNT5A and measure fluorescence by flow cytometry. Alternatively, use surface plasmon resonance (SPR) with immobilized Frizzled-2 or ROR1 receptor extracellular domains.
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| Cell Assay |
Culture DU145, PC3, or MDA-MB-231 breast cancer cells in DMEM with 10% FBS. For invasion assays, coat Transwell inserts with Matrigel. Add serum-free medium containing Foxy-5 TFA (100 uM) to the upper chamber and medium with 10% FBS as chemoattractant to the lower chamber. Seed cells (1 × 10^5) in the upper chamber. Incubate for 24 hours at 37degC. Stain invaded cells with crystal violet and count under a microscope. For calcium signaling assays, load cells with Fluo-4 AM, add Foxy-5 (1-100 uM), and measure fluorescence (ex/em 494/516 nm) using a plate reader. For migration (scratch) assays, create a wound in confluent cell monolayers and add Foxy-5 (10-100 uM). Monitor wound closure at 0, 6, 12, and 24 hours.
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| Animal Protocol |
For orthotopic prostate cancer models, use immunodeficient mice. Inject WNT5A-low DU145 prostate cancer cells orthotopically into the prostate. After tumor establishment, administer Foxy-5 TFA via intraperitoneal injection at 2 mg/kg, once daily for 3-9 weeks. Monitor tumor growth by bioluminescence imaging or caliper measurement. At sacrifice, examine lymph nodes and lungs for metastatic lesions. For xenograft colon cancer models, inject human colon cancer cells subcutaneously or orthotopically. Administer Foxy-5 (2 mg/kg i.p., 9 times/day for 7-23 days). Collect tumors for immunohistochemistry to assess ALDH, DCLK1, COX-2, and 15-PGDH expression by Western blot or IHC. For breast cancer metastasis models, use the 4T1 syngeneic model or MDA-MB-231 xenografts. Administer Foxy-5 (2 mg/kg i.p., 3-5 times/week). Assess lung metastasis by histological examination after staining with H&E or by quantifying metastatic nodules.
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| ADME/Pharmacokinetics |
Foxy-5 is a hexapeptide (MW 808.80) with the sequence For-MDGCEL (formylated Met-Asp-Gly-Cys-Glu-Leu). As a peptide, it is subject to proteolytic degradation in circulation. The TFA salt enhances solubility. For in vivo use, dissolve in PBS (7.14 mg/mL, 8.83 mM) or saline (5 mg/mL, 6.18 mM) with sonication. The compound is administered intraperitoneally at 2 mg/kg. Storage: Powder at -20degC up to 2 years, -80degC for 2 years; in solvent at -80degC for 6 months or -20degC for 1 month, sealed, away from moisture.
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| Toxicity/Toxicokinetics |
Foxy-5 TFA has a favorable safety profile in preclinical studies. At the effective dose of 2 mg/kg administered intraperitoneally in mice, no significant acute toxicity or adverse effects have been reported in published studies. The compound targets WNT5A signaling and reduces cancer cell migration without affecting normal cell viability. No genotoxicity or carcinogenicity data are available. The TFA salt may cause irritation; standard laboratory precautions (gloves, lab coat, safety glasses) should be used.
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| References |
[1]. Säfholm A, et al. The Wnt-5a-derived hexapeptide Foxy-5 inhibits breast cancer metastasis in vivo by targeting cell motility. Clin Cancer Res. 2008 Oct 15;14(20):6556-63.
[2]. Osman J, et al. The WNT5A Agonist Foxy5 Reduces the Number of Colonic Cancer Stem Cells in a Xenograft Mouse Model of Human Colonic Cancer. Anticancer Res. 2019 Apr;39(4):1719-1728. [3]. Canesin G, et al. Treatment with the WNT5A-mimicking peptide Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model. PLoS One. 2017 Sep 8;12(9):e0184418. [4]. Kelsey R. Prostate cancer: Foxy-5 in prostate cancer model. Nat Rev Urol. 2017 Nov;14(11):638. |
| Additional Infomation |
Foxy-5 TFA has been investigated in preclinical models for the treatment of metastatic breast cancer, prostate cancer, and colorectal cancer. The compound was originally developed from WNT5A-derived hexapeptide research. Clinical development has included Phase I studies in cancer patients. Foxy-5 is covered by patents and is exclusively for research use. The compound is also known as Foxy5 or Foxy-5. For research use only; not for diagnostic or therapeutic applications.
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| Molecular Formula |
C28H43F3N6O14S2
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|---|---|
| Molecular Weight |
808.80
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| Related CAS # |
Foxy-5;881188-51-8
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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) |
H2O :~20 mg/mL (~24.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 7.14 mg/mL (8.83 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2364 mL | 6.1820 mL | 12.3640 mL | |
| 5 mM | 0.2473 mL | 1.2364 mL | 2.4728 mL | |
| 10 mM | 0.1236 mL | 0.6182 mL | 1.2364 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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