| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
The primary target of m-PEG15-amine is not a biological receptor but rather chemical functional groups. 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 allows it to serve as a linker in bioconjugation strategies, facilitating the attachment of drugs or other molecules to target biomolecules.
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| ln Vitro |
One ligand is for an E3 ubiquitin ligase, and the other is for the target protein; these two ligands are joined by a linker to form PROTACs. The intracellular ubiquitin-proteasome system is utilized by PROTACs to specifically destroy target proteins[1].
As a chemical linker, m-PEG15-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 PEG15 spacer provides excellent hydrophilicity and flexibility, which can improve the pharmacokinetic properties of the final conjugate by increasing its solubility and reducing its immunogenicity. |
| ln Vivo |
No direct in vivo activity is attributed to m-PEG15-amine itself. Its role is as a component in larger therapeutic constructs, such as ADCs and PROTACs. In these molecules, the PEG15 linker provides the appropriate distance and flexibility between the two functional components. For example, mPEG-amine (MW 4000) has been used to synthesize folic acid-conjugated polymer micelles for encapsulating anticancer compounds.
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| Enzyme Assay |
For in vitro characterization, m-PEG15-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-PEG15-amine itself. As a linker, it is incorporated into larger constructs (e.g., polymer micelles, ADCs, or PROTACs) that are then evaluated in cell culture. For example, polymer micelles containing this linker would be tested for their ability to deliver an encapsulated drug to cancer cells and induce cell death.
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| Animal Protocol |
In vivo studies with m-PEG15-amine are conducted using the final conjugate (e.g., polymer micelles, ADCs, or PROTACs). These studies typically involve administering the conjugate to animal models to assess its pharmacokinetics, efficacy, and safety. The PEG15 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-PEG15-amine does not have independent pharmacokinetic (PK) properties. However, the PEG15 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-PEG15-amine is not typically evaluated independently. PEG is generally considered to be biocompatible and non-toxic.
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| References | |
| Additional Infomation |
m-PEG15-amine is a linear, heterobifunctional PEG linker with a methoxy group and a primary amine group. It has a molecular weight of 559.7 g/mol and is used for bioconjugation to improve the solubility and pharmacokinetics of therapeutic agents. The amine group provides a reactive handle for conjugation to carboxylic acids and activated esters. 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 |
559.6878
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| Exact Mass |
559.357
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| CAS # |
80506-64-5
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| Related CAS # |
m-PEG2000-NH2 hydrochloride
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| PubChem CID |
51340958
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| Appearance |
White to light yellow solid powder
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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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| Melting Point |
58-61 °C(lit.)
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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 |
C(CN)O{-}CC{+n}OC
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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: 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) |
DMSO: ~100 mg/mL (with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (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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