| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PEGs
PROTAC Linkers. |
|---|---|
| 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 PEGylation reagent, m-PEG24-Mal itself has no intrinsic biological activity; it is used to modify thiol groups on proteins, peptides, or small molecules to improve their physicochemical and pharmacokinetic properties. The maleimide group undergoes Michael addition with thiols at pH 6.5-7.5 to form a stable thioether linkage. The long PEG24 chain provides a hydrophilic shield that can reduce protein aggregation, decrease immunogenicity, and prolong circulation half-life by reducing renal clearance and protecting against proteolytic degradation. In PROTAC research, this reagent can be used to PEGylate a target protein ligand or an E3 ligase ligand to improve its solubility and stability before incorporation into a PROTAC, or to PEGylate a complete PROTAC molecule to enhance its pharmacokinetic properties. |
| ln Vivo |
No specific in vivo activity has been reported for this PEGylation reagent alone; its activity is derived from the final PEGylated conjugate.
|
| Enzyme Assay |
N/A; this compound is not assessed in isolated enzyme/receptor binding assays. As a PEGylation reagent, its quality is typically confirmed by analytical methods such as HPLC and NMR. The molecular weight distribution (polydispersity) of the PEG24 chain is typically characterized by GPC or MALDI-TOF mass spectrometry. The maleimide content is typically determined by titration with a thiol-containing compound (e.g., cysteine) and measuring the residual thiols with Ellman's reagent, or by UV absorption at 300 nm. The compound is often used as a reference standard.
|
| Cell Assay |
N/A; this linker is not tested alone in cell-based assays. In a typical PEGylation reaction, the maleimide group is reacted with a thiol-containing molecule (e.g., a PROTAC molecule containing a free thiol, or a cysteine-containing protein) in a buffer such as PBS (pH 6.5-7.5) at room temperature for 1-4 hours. The PEGylated product is then purified and tested in cells for its biological activity. For example, PEGylation of a PROTAC may improve its cellular uptake or reduce non-specific binding. The effect of PEGylation on target degradation activity is assessed by Western blotting.
|
| Animal Protocol |
N/A; no animal studies are performed with the PEGylation reagent alone. For a PEGylated conjugate, in vivo studies are conducted following institutional guidelines. The long PEG24 chain is expected to significantly prolong the circulation half-life, reduce immunogenicity, and improve the pharmacokinetic properties of the conjugate. The PEGylated conjugate is typically formulated in a suitable vehicle (e.g., PBS) and administered via intravenous (IV) injection.
|
| ADME/Pharmacokinetics |
This compound has a molecular weight of approximately 1239.44, a molecular formula of C56H106N2O27, and a standard purity of ≥93-95%. For storage, it should be kept as a powder at -20degC for up to 3 years, protected from light and moisture. It is soluble in DMSO and other organic solvents. The product should be stored in a sealed container under an inert atmosphere (e.g., nitrogen) to prevent hydrolysis of the maleimide group. The compound is also known as mPEG24-maleimide and Methyl-PEG24-Maleimide. CAS: 2579693-28-8.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human or veterinary use. Standard chemical safety precautions should be observed during handling. The maleimide group is moisture-sensitive and should be handled in a dry environment. It is not an approved therapeutic drug and has not been cleared for clinical use. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
|
| References |
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
|
| Additional Infomation |
The extremely long PEG24 maleimide provides an exceptionally long, flexible, and hydrophilic PEG chain for site-specific PEGylation of thiol-containing molecules. This reagent is widely used in the PEGylation of therapeutic proteins to reduce immunogenicity and improve pharmacokinetic properties, as well as in the preparation of PEGylated nanoparticles and liposomes for drug delivery. In PROTAC research, it can be used to improve the solubility and pharmacokinetic properties of PROTACs, which often suffer from poor aqueous solubility and rapid clearance. The maleimide group provides a specific conjugation handle for thiols, enabling the site-specific attachment of the PEG chain to a cysteine residue in a protein or to a thiol-functionalized small molecule. The long PEG24 chain provides a dense hydrophilic corona that effectively shields the conjugated molecule from immune recognition and reduces renal clearance.
|
| Molecular Formula |
C56H106N2O27
|
|---|---|
| Molecular Weight |
1239.43806123734
|
| Exact Mass |
1238.698
|
| CAS # |
2579693-28-8
|
| PubChem CID |
91757738
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-3.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
27
|
| Rotatable Bond Count |
75
|
| Heavy Atom Count |
85
|
| Complexity |
1400
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1(CCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C(=O)C=CC1=O
|
| InChi Key |
IRQWFNZIEAPTBJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C56H106N2O27/c1-62-8-9-64-12-13-66-16-17-68-20-21-70-24-25-72-28-29-74-32-33-76-36-37-78-40-41-80-44-45-82-48-49-84-52-53-85-51-50-83-47-46-81-43-42-79-39-38-77-35-34-75-31-30-73-27-26-71-23-22-69-19-18-67-15-14-65-11-10-63-7-5-57-54(59)4-6-58-55(60)2-3-56(58)61/h2-3H,4-53H2,1H3,(H,57,59)
|
| Chemical Name |
3-(2,5-dioxopyrrol-1-yl)-N-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]propanamide
|
| 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)
|
| Solubility (In Vitro) |
DMSO :~100 mg/mL (~80.68 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (2.02 mM) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8068 mL | 4.0341 mL | 8.0682 mL | |
| 5 mM | 0.1614 mL | 0.8068 mL | 1.6136 mL | |
| 10 mM | 0.0807 mL | 0.4034 mL | 0.8068 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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