| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
As a PEG-based linker rather than a pharmacologically active drug, Amino-PEG9-acid does not possess a defined biological target or receptor. Its role is to serve as a stable, non-cleavable structural bridge between antibodies and cytotoxic payloads in ADCs, or between E3 ubiquitin ligase ligands and target protein ligands in PROTACs. The amino group provides a handle for conjugation to antibodies or target-binding ligands, while the carboxylic acid group enables attachment to drug payloads or E3 ligase ligands via amide bond formation. The non-cleavable nature ensures conjugate stability during systemic circulation.
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| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC.
In vitro, Amino-PEG9-acid functions as a non-cleavable ADC linker that enables stable attachment of cytotoxic agents to monoclonal antibodies. ADCs consist of an antibody linked to an ADC cytotoxin via an ADC linker. The non-cleavable linker forms a stable bond that offers stability to the conjugate during circulation and helps enhance the therapeutic efficacy of the ADC in targeted therapy approaches. The hydrophilic PEG spacer improves aqueous solubility of the conjugate, reduces aggregation, and minimizes nonspecific interactions. In PROTAC applications, the linker connects the two functional ligands to enable ternary complex formation. |
| ln Vivo |
In vivo, Amino-PEG9-acid is not a therapeutic agent itself but a chemical component used in the construction of biopharmaceuticals. The resulting ADC conjugates incorporating this non-cleavable PEG linker are designed for in vivo administration to achieve targeted cancer therapy. The non-cleavable nature of the linker ensures that the cytotoxic payload remains attached to the antibody until the entire ADC is internalized and degraded within the target cell, releasing the active drug intracellularly. This mechanism can enhance therapeutic efficacy and reduce systemic toxicity. The PEG spacer improves pharmacokinetic properties by increasing hydrodynamic volume and reducing renal clearance.
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| Enzyme Assay |
For in vitro enzyme/receptor binding studies, Amino-PEG9-acid is typically evaluated as part of an ADC construct rather than as a standalone compound. The linker’s stability and lack of cleavage can be verified by HPLC or mass spectrometry. Binding affinity of the complete ADC to its target antigen can be assessed using surface plasmon resonance (SPR) or enzyme-linked immunosorbent assay (ELISA). The efficiency of ADC internalization and intracellular payload release can be evaluated using fluorescence-based assays or LC-MS/MS quantification of released drug. These methods are for reference only and require independent validation.
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| Cell Assay |
In vitro cell-based assays for Amino-PEG9-acid involve testing the biological activity of the complete ADC conjugate. Standard protocols include cell viability assays (e.g., MTT, CCK-8, or CellTiter-Glo) performed on target antigen-expressing cancer cell lines to assess cytotoxicity and determine IC₅₀ values. Cells are typically cultured in appropriate media with 10% FBS at 37°C in 5% CO₂ and treated with serial dilutions of the ADC for 48-96 hours. Internalization assays using fluorescently labeled antibodies and confocal microscopy can evaluate receptor-mediated uptake. Flow cytometry can assess target antigen expression levels and binding efficiency.
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| Animal Protocol |
In vivo animal studies using Amino-PEG9-acid are conducted with the final ADC conjugate. Typical protocols involve xenograft mouse models bearing human tumor cells to evaluate antitumor efficacy. Dosing regimens often include intravenous administration at 1-10 mg/kg, administered weekly or biweekly, to assess tumor growth inhibition, survival benefit, and pharmacokinetics. Formulation preparation typically involves dissolving the compound in DMSO followed by dilution with PEG300, Tween 80, and saline or PBS. Tumor volumes are measured regularly using calipers, and body weight is monitored for toxicity assessment. Pharmacodynamic endpoints include target engagement and biomarker modulation in tumor tissues.
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| ADME/Pharmacokinetics |
As a PEG linker rather than a drug, Amino-PEG9-acid does not have intrinsic pharmacokinetic properties. However, PEG linkers contribute to the pharmacokinetic profile of ADCs by increasing hydrodynamic radius, reducing renal filtration, and prolonging circulation half-life. The non-cleavable nature of this linker ensures that the drug remains conjugated to the antibody during circulation, minimizing premature drug release and associated systemic toxicity. The pharmacokinetics of the final ADC depend on multiple factors including the antibody, payload, conjugation site, and drug-to-antibody ratio, with typical half-lives ranging from several days to weeks in preclinical species.
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| Toxicity/Toxicokinetics |
As a chemical linker not intended for direct therapeutic use, Amino-PEG9-acid has limited toxicity data available. The compound is classified for research use only and not for human consumption. General safety precautions for handling PEG-based reagents apply, including the use of personal protective equipment and working in a fume hood. The final ADC conjugates incorporating this linker undergo extensive toxicological evaluation in preclinical species (e.g., rats and cynomolgus monkeys) to assess maximum tolerated dose, target organ toxicity, and off-target effects prior to clinical development.
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| References |
[1]. Iwaoka E, et al. Improvement of monolithic solid material by utilization of spacer for identification of the target using affinity resins. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1469-72.
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| Additional Infomation |
Additional information: Amino-PEG9-acid is sensitive to light and moisture. The density is 1.127 g/cm³ (predicted). Storage conditions: powder at -20°C for up to 3 years; in solvent at -80°C for up to 1 year. This compound is part of a family of PEG linkers with varying ethylene glycol unit lengths that allow fine-tuning of solubility, flexibility, and pharmacokinetic properties. The product is for research and drug registration purposes only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C21H43NO11
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|---|---|
| Molecular Weight |
485.566228151321
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| Exact Mass |
485.283
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| CAS # |
1191079-83-0
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| PubChem CID |
122361149
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| Appearance |
White to light yellow Solid-Liquid Mixture
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
578.3±50.0 °C at 760 mmHg
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| Flash Point |
303.6±30.1 °C
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| Vapour Pressure |
0.0±3.5 mmHg at 25°C
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| Index of Refraction |
1.470
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| LogP |
-3.71
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
33
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| Complexity |
391
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOCCOCCN)CCOCCOCCOCCOCCC(=O)O
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| InChi Key |
ZYPBFSLIVZGGED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H43NO11/c22-2-4-26-6-8-28-10-12-30-14-16-32-18-20-33-19-17-31-15-13-29-11-9-27-7-5-25-3-1-21(23)24/h1-20,22H2,(H,23,24)
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| Chemical Name |
3-[2-[2-[2-[2-[2-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoic acid
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 2.0594 mL | 10.2972 mL | 20.5944 mL | |
| 5 mM | 0.4119 mL | 2.0594 mL | 4.1189 mL | |
| 10 mM | 0.2059 mL | 1.0297 mL | 2.0594 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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