| Size | Price | |
|---|---|---|
| Other Sizes |
Purity: ≥98%
| Targets |
The primary targets of Amino-PEG2-acid are the functional groups on biomolecules that it conjugates to, rather than specific biological receptors. The amine group (-NH2) is reactive with carboxylic acids, activated NHS esters, and carbonyl groups (ketones, aldehydes), enabling the formation of stable amide or imine bonds. The terminal carboxylic acid (-COOH) can be activated (e.g., with EDC or DCC) to react with primary amine groups on proteins, peptides, or other biomolecules, forming stable amide bonds. As a PEG-based linker, it facilitates the attachment of therapeutic agents to target biomolecules, enhancing their stability and efficacy in therapeutic applications.
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| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC. Two distinct ligands, one for the E3 ubiquitin ligase and the other for the target protein, are present in PROTAC and are joined by a linker. PROTAC targets and selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system.
In vitro, Amino-PEG2-acid is used as a building block for the synthesis of bioconjugates rather than as a directly active biological agent. The compound's primary in vitro application is in bioconjugation chemistry, where it serves as a versatile linker to attach various biomolecules such as proteins, peptides, and small molecules. The PEG spacer enhances the solubility and stability of the resulting conjugates in aqueous solutions. Studies have demonstrated that the compound can effectively bind to various cellular targets through its conjugated payloads, influencing cellular processes. In PROTAC synthesis, the linker connects the target protein ligand to the E3 ligase ligand, enabling targeted protein degradation. |
| ln Vivo |
In vivo, Amino-PEG2-acid is not administered directly as a therapeutic agent but is used to synthesize PROTACs, ADCs, and other bioconjugates that are evaluated in animal models. The PEG spacer enhances the solubility, stability, and bioavailability of the resulting conjugates, improving their pharmacokinetic properties. The compound's role as a linker in ADC synthesis enables targeted delivery of chemotherapeutics with reduced systemic toxicity. In PROTAC development, the PEG linker facilitates the formation of chimeric molecules that induce degradation of disease-relevant proteins. The compound's utility in drug development has been validated in various preclinical studies involving animal models of cancer and other diseases.
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| Enzyme Assay |
In cell-free biochemical assays, Amino-PEG2-acid is characterized for its chemical properties and conjugation efficiency. The compound's purity (>98%) and molecular weight (177.20 g/mol, formula C7H15NO4) are determined using analytical techniques such as HPLC and mass spectrometry. Its reactivity with carboxylic acids, NHS esters, and carbonyls is assessed to ensure compatibility with conjugation reactions. The compound's solubility in aqueous and organic solvents is evaluated to determine optimal reaction conditions for bioconjugation. Stability studies under various storage conditions are conducted to ensure the integrity of the linker for long-term research use.
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| Cell Assay |
In cellular assays, Amino-PEG2-acid is evaluated indirectly through the biological activity of the conjugates synthesized using this linker. The resulting PROTACs are tested for their ability to degrade target proteins in cell lines, with the PEG linker's effect on cellular uptake, intracellular trafficking, and protein degradation activity being assessed. The resulting ADCs are evaluated for their ability to bind to target antigens, mediate internalization, and deliver cytotoxic payloads to cancer cells. The PEG linker's impact on cell permeability and bioavailability is characterized in relevant cell models. The compound itself is not biologically active and serves only as a structural component.
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| Animal Protocol |
Animal models for Amino-PEG2-acid involve evaluating the PROTACs or ADCs synthesized using this linker in preclinical studies. The resulting conjugates are tested in tumor xenograft models (for ADCs) or disease models relevant to the target protein (for PROTACs). The PEG linker's effect on pharmacokinetics, biodistribution, and efficacy is assessed. Studies have examined the compound's role in enabling targeted drug delivery and protein degradation in various animal models. The compound's ability to enhance the solubility and stability of therapeutic conjugates has been demonstrated in pharmacokinetic and efficacy studies in rodents.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Amino-PEG2-acid are not typically reported, as the compound is a linker rather than a therapeutic agent. However, the PEG moiety contributes to the favorable pharmacokinetic properties of the resulting conjugates, including enhanced solubility, reduced immunogenicity, and prolonged circulation time. The compound has a molecular weight of 177.20 g/mol with a molecular formula of C7H15NO4. The CAS number is 791028-27-8. The compound is soluble in water and common organic solvents. It should be stored at -20°C for long-term stability. Standard handling procedures for PEG linkers apply.
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| Toxicity/Toxicokinetics |
The toxicity profile of Amino-PEG2-acid is not extensively documented, as the compound is a linker rather than a pharmacologically active agent. The compound is supplied at ≥95% purity and is intended for research use only. Standard safety precautions for handling laboratory chemicals apply, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound is not intended for human use or therapeutic applications. As with all chemical reagents, appropriate handling and disposal procedures should be followed to minimize exposure and environmental impact.
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| References | |
| Additional Infomation |
Amino-PEG2-acid is a heterobifunctional PEG linker extensively used in the synthesis of PROTACs, ADCs, and other bioconjugates. It is a non-cleavable linker containing an amine group and a carboxylic acid group linked through a linear PEG chain. The amine group enables conjugation to carboxylic acids and activated esters, while the carboxylic acid group enables conjugation to amines. The PEG spacer enhances solubility and reduces aggregation of conjugated biomolecules. The compound is widely used in bioconjugation, drug development, surface modification, and cellular interaction studies. Its applications extend to medical research, drug delivery, nanotechnology, and new materials research. The CAS number is 791028-27-8.
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| Molecular Formula |
C7H15NO4
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|---|---|
| Molecular Weight |
177.1983
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| Exact Mass |
177.1
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| CAS # |
791028-27-8
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| Related CAS # |
791028-27-8;
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| PubChem CID |
14462391
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
331.5±27.0 °C at 760 mmHg
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| Flash Point |
154.3±23.7 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.467
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| LogP |
-1.21
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
12
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| Complexity |
118
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(COCCOCCN)C(=O)O
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| InChi Key |
DEZXLFKSYRODPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H15NO4/c8-2-4-12-6-5-11-3-1-7(9)10/h1-6,8H2,(H,9,10)
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| Chemical Name |
3-[2-(2-aminoethoxy)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 |
| 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 | 5.6433 mL | 28.2167 mL | 56.4334 mL | |
| 5 mM | 1.1287 mL | 5.6433 mL | 11.2867 mL | |
| 10 mM | 0.5643 mL | 2.8217 mL | 5.6433 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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