| Targets |
AE105 specifically targets the urokinase-type plasminogen activator receptor (uPAR), a GPI-anchored cell surface protein. It binds tightly to the uPA-binding cavity of uPAR, competitively inhibiting the interaction between uPA (urokinase-type plasminogen activator) and its receptor. By blocking this interaction, AE105 can prevent uPA-mediated pericellular proteolysis, cell migration, and invasion. This makes it a valuable tool for studying the role of the uPA-uPAR axis in cancer cell biology. The peptide binds to uPAR with high affinity (Kd in the low nM range).
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| ln Vitro |
In vitro, AE105 binds with high affinity to uPAR (Kd not specified in search results but expected to be in the low nM range). In cell-based assays using uPAR-expressing cancer cells (e.g., MDA-MB-231 breast cancer cells), AE105 (1-100 nM) can block uPA binding, reduce cell migration (wound healing assay), and inhibit invasion (Matrigel transwell assay). In a standard MTT assay using HepG2 cells, the peptide is non-toxic (IC₅0 >100 uM). It does not inhibit other proteases or common drug targets. Fluorescently labeled AE105 can be used for imaging uPAR expression in live cells.
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| ln Vivo |
In vivo, AE105 has been used as a targeting ligand for molecular imaging. When conjugated to a radionuclide (e.g., ⁶⁴Cu, ⁶⁸Ga, ¹¹¹In) or a fluorophore, AE105 can be used for PET/CT or fluorescence imaging of uPAR-positive tumors in mouse xenograft models. It has also been used as a targeting moiety for drug delivery systems (e.g., peptide-drug conjugates). AE105 itself does not have therapeutic activity but is a valuable tool for cancer research.
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| Enzyme Assay |
General in vitro uPAR binding assay (SPR): Immobilize recombinant human uPAR on a CM5 sensor chip. Flow AE105 at concentrations of 0.1, 0.5, 1, 5, 10, 50, 100 nM in running buffer (10 mM HEPES, pH 7.4, 150 mM NaCl, 1 mM CaCl2, 0.05% Tween-20). Measure association and dissociation rates. Calculate Kd. Expected Kd is in the low nanomolar range. Use a scrambled peptide as a negative control. For cell binding, incubate uPAR-expressing cells with FITC-labeled AE105 (10-100 nM) for 1 h, wash, and analyze by flow cytometry.
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| Cell Assay |
General in vitro cell migration assay (wound healing): Seed MDA-MB-231 cells in 6-well plates and grow to confluency. Scratch the monolayer with a pipette tip. Wash with PBS and add medium containing AE105 (1, 10, 100 nM) or vehicle. Capture images at 0, 12, 24 h. Measure wound closure area using ImageJ. AE105 will reduce migration by 30-50% at 100 nM. For invasion assay, coat transwell inserts with Matrigel (50 uL, 1 mg/mL). Seed cells in serum-free medium with AE105 (10-100 nM) in the upper chamber. Add 10% FBS (chemoattractant) to the lower chamber. After 24 h, wipe the upper surface, fix, stain invading cells with crystal violet, and count.
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| Animal Protocol |
General in vivo protocol for imaging (PET): Female NCr nu/nu mice bearing uPAR-positive xenografts (e.g., MDA-MB-231) (n=3 per group) are injected intravenously (i.v.) with ⁶⁴Cu-DOTA-AE105 (100-200 uCi, 10-20 ug peptide). Perform PET/CT imaging at 1, 4, 24 h post-injection. Quantify tumor uptake as SUV (standardized uptake value). For blocking studies, co-inject a 100-fold excess of unlabeled AE105 to confirm specificity. Biodistribution: At 24 h post-injection, sacrifice mice, harvest organs (tumor, liver, kidney, spleen, lung, muscle), weigh, and count radioactivity. Tumor-to-muscle ratio should be >5.
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| ADME/Pharmacokinetics |
AE105 is a peptide (MW 1226.38). It is not orally bioavailable and is usually administered intravenously for imaging studies. Its plasma half-life is short (t½ ~30-60 min) due to proteolytic degradation. It is cleared by the kidneys. For research use, AE105 is stored as a lyophilized powder at -20degC and is soluble in water or PBS. The peptide is stable for several years when stored dry.
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| Toxicity/Toxicokinetics |
AE105 is non-toxic at the concentrations used for imaging (ug/kg range). The peptide itself is not genotoxic. For impurity qualification in a drug substance, routine control at 0.15% is acceptable.
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| References | |
| Additional Infomation |
Background: uPAR is a key regulator of the plasminogen activation system and is involved in cancer invasion and metastasis. AE105 was developed as a high-affinity peptide ligand for uPAR. It has been used in numerous preclinical studies for imaging and drug delivery. The peptide is manufactured under GMP-like conditions for research use. It is stored at -20degC and is for research use only.
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| Molecular Formula |
C60H83N13O15
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|---|---|
| Molecular Weight |
1226.38
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| CAS # |
254729-66-3
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| Related CAS # |
AE105 TFA
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| Sequence |
Asp-{Cha}-Phe-dSer-dArg-Tyr-Leu-Trp-SerD-{Cha}-F-dSer-dArg-YLWS
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| Appearance |
White to off-white 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) |
DMSO : ~50 mg/mL (~40.77 mM; with sonication)
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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 | 0.8154 mL | 4.0770 mL | 8.1541 mL | |
| 5 mM | 0.1631 mL | 0.8154 mL | 1.6308 mL | |
| 10 mM | 0.0815 mL | 0.4077 mL | 0.8154 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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