| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
The primary target of m-PEG12-amine is not a biological receptor but rather chemical functional groups on other molecules. The terminal primary amine (-NH₂) is the key reactive moiety. It reacts with carboxylic acids in the presence of coupling agents (e.g., EDC, HOBt) to form stable amide bonds. It also reacts with activated esters, such as N-hydroxysuccinimide (NHS) esters, to form amide linkages. This reactivity makes it a versatile linker for bioconjugation. In ADCs and PROTACs, it serves to connect the targeting or functional moiety to the payload or ligand.
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| ln Vitro |
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 selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system [1]. ADC is made up of antibodies that are connected to ADC cytotoxins by an ADC linker [2].
As a chemical linker, m-PEG12-amine has no intrinsic biological activity. Its utility is derived from its chemical reactivity. The amine group can be used to conjugate the PEG chain to a wide variety of molecules, including antibodies, drugs, and ligands. The long PEG12 spacer provides excellent hydrophilicity and flexibility, which can improve the pharmacokinetic properties of the final conjugate by increasing its solubility and reducing its immunogenicity. The compound is non-cleavable, meaning the linker is designed to be stable in the biological environment. |
| ln Vivo |
No direct in vivo activity is attributed to m-PEG12-amine itself. Its role is as a component in larger therapeutic constructs. In ADCs, the PEG12 linker connects the antibody to the cytotoxic drug, helping to improve the drug's solubility and stability in circulation. In PROTACs, it connects the target protein ligand to the E3 ubiquitin ligase ligand, providing the necessary spatial arrangement for the PROTAC to function.
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| Enzyme Assay |
For in vitro characterization, m-PEG12-amine is typically analyzed by NMR and HPLC to confirm its structure and purity. Purity is often >98%. The amine content can be quantified by titration or by derivatization with a reagent such as ninhydrin or fluorescamine. Its solubility in various solvents is determined, as it is important for its use in conjugation reactions.
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| Cell Assay |
Cell-based assays are not performed on m-PEG12-amine alone. As a linker, it is incorporated into larger constructs (ADCs or PROTACs) that are then evaluated in cell culture. For example, an ADC containing the m-PEG12-amine linker would be tested for its ability to bind to cancer cells, be internalized, and deliver a cytotoxic payload. The efficacy of the ADC would be assessed by measuring cell viability.
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| Animal Protocol |
In vivo studies with m-PEG12-amine are conducted using the final conjugate (ADC or PROTAC). These studies typically involve administering the conjugate to animal models, such as tumor-bearing mice, to assess its pharmacokinetics, efficacy, and safety. The PEG12 spacer contributes to the favorable pharmacokinetic profile of the conjugate by increasing its solubility and reducing its clearance.
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| ADME/Pharmacokinetics |
As a linker, m-PEG12-amine does not have independent pharmacokinetic (PK) properties. However, the PEG12 spacer is known to improve the PK of the final conjugate. The hydrophilic PEG chain reduces opsonization and clearance by the immune system, leading to a longer circulation half-life. This can result in improved drug exposure to the target tissue and enhanced efficacy.
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| Toxicity/Toxicokinetics |
The toxicology of m-PEG12-amine is not typically evaluated independently. PEG is generally considered to be biocompatible and non-toxic. The compound is a non-cleavable linker, meaning it is designed to be stable and not metabolized, which contributes to its low inherent toxicity.
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| References | |
| Additional Infomation |
m-PEG12-amine is a non-cleavable, 12-unit PEG linker used in the synthesis of ADCs and PROTACs. It has a molecular weight of 559.69 g/mol and features a primary amine group for conjugation. The long, hydrophilic PEG12 spacer enhances the solubility and stability of bioconjugates. It is a valuable tool for drug delivery and targeted therapy research, available for research use only.
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| Molecular Formula |
C25H53NO12
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|---|---|
| Molecular Weight |
559.687829732895
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| Exact Mass |
559.356
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| CAS # |
1977493-48-3
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| PubChem CID |
51340958
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
583.6±45.0 °C at 760 mmHg
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| Flash Point |
291.3±22.4 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.458
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| LogP |
-4.59
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
35
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| Heavy Atom Count |
38
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| Complexity |
413
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOCCOCCOCCN)CCOCCOCCOCCOCCOCCOC
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| InChi Key |
MSKSQCLPULZWNO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H53NO12/c1-27-4-5-29-8-9-31-12-13-33-16-17-35-20-21-37-24-25-38-23-22-36-19-18-34-15-14-32-11-10-30-7-6-28-3-2-26/h2-26H2,1H3
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| Chemical Name |
2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanamine
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 : ~100 mg/mL (~178.67 mM)
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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 | 1.7867 mL | 8.9335 mL | 17.8670 mL | |
| 5 mM | 0.3573 mL | 1.7867 mL | 3.5734 mL | |
| 10 mM | 0.1787 mL | 0.8934 mL | 1.7867 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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