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Foxy-5 is a novel, peptide-mimicking and potent wnt signalling pathway modulator with the potential to be used forthe treatment of cancer.
| ln Vivo |
In an orthotopic mouse model, Foxy-5 efficiently inhibits the metastatic spread of WNT5A-low prostate cancer cells [1]. In human colon cancer xenograft mouse models, Foxy-5 decreases the quantity of colon cancer stem cells [2].
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| References |
[1]. 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.
[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 |
(2S)-2-[[(2S)-4-carboxy-2-[[(2R)-2-[[2-[[(2S)-3-carboxy-2-[[(2S)-2-formamido-4-(methylthio)-1-oxobutyl]amino]-1-oxopropyl]amino]-1-oxoethyl]amino]-3-mercapto-1-oxopropyl]amino]-1-oxobutyl]amino]-4-methylpentanoic acid is a peptide.
Foxy-5 has been used in trials studying the treatment of Prostate Cancer, Colorectal Cancer, Metastatic Colon Cancer, Metastatic Breast Cancer, and Metastatic Prostate Cancer. Wnt-5a Mimic Hexapeptide Foxy-5 is a formylated, six amino acid, Wnt5a-derived peptide and wnt-5a mimetic with potential anti-metastatic activity. Upon intravenous administration, Wnt-5a mimic hexapeptide foxy-5 binds to and activates the wnt-5a receptors, Frizzled-2 and -5, which activates wnt-5a-mediated signaling. Increased wnt-5a signaling may inhibit endothelial tumor cell migration and invasion. This may decrease metastasis of susceptible tumor cells. However, foxy-5 does not affect tumor cell proliferation or apoptosis. Foxy-5 lacks a heparan sulfate-binding domain and contains a formyl group on its NH2-terminal methionine residue which decreases in vivo degradation. Decreased expression of wnt-5a protein is associated with increased motility of certain tumor cell types. |
| Molecular Formula |
C26H42N6O12S2
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|---|---|
| Molecular Weight |
694.772
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| Exact Mass |
694.23
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| CAS # |
881188-51-8
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| Related CAS # |
Foxy-5 TFA
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| PubChem CID |
44628955
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1244.1±65.0 °C at 760 mmHg
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| Flash Point |
706.2±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.562
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| LogP |
0.62
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
46
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(C)C[C@@H](C(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC=O
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| InChi Key |
WFZPJYYCTSHDJI-ATIWLJMLSA-N
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| InChi Code |
InChI=1S/C26H42N6O12S2/c1-13(2)8-17(26(43)44)32-24(41)15(4-5-20(35)36)30-25(42)18(11-45)29-19(34)10-27-22(39)16(9-21(37)38)31-23(40)14(28-12-33)6-7-46-3/h12-18,45H,4-11H2,1-3H3,(H,27,39)(H,28,33)(H,29,34)(H,30,42)(H,31,40)(H,32,41)(H,35,36)(H,37,38)(H,43,44)/t14-,15-,16-,17-,18-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-4-carboxy-2-[[(2R)-2-[[2-[[(2S)-3-carboxy-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]propanoyl]amino]acetyl]amino]-3-sulfanylpropanoyl]amino]butanoyl]amino]-4-methylpentanoic acid
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| Synonyms |
Foxy5 Foxy 5 Foxy-5
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4393 mL | 7.1966 mL | 14.3933 mL | |
| 5 mM | 0.2879 mL | 1.4393 mL | 2.8787 mL | |
| 10 mM | 0.1439 mL | 0.7197 mL | 1.4393 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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