| 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 linker molecule, m-PEG37-acid itself has no intrinsic biological activity; it serves as a structural connector to join a target protein ligand and an E3 ubiquitin ligase ligand in PROTAC synthesis. The long PEG chain imparts high hydrophilicity and flexibility to the PROTAC molecule, which can facilitate the formation of a productive ternary complex between the target protein, the PROTAC, and the E3 ligase. PEG linkers are known to improve the solubility, reduce aggregation, and extend the circulation half-life of bioconjugates. The terminal carboxylic acid allows for amide bond formation with amine-containing ligands using standard coupling reagents such as EDC and NHS. |
| ln Vivo |
No specific in vivo activity has been reported for this linker alone; its activity is derived from the final PROTAC molecule after conjugation with appropriate ligands. The in vivo efficacy of a complete PROTAC is determined in animal models.
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| Enzyme Assay |
N/A; this compound is not assessed in isolated enzyme/receptor binding assays. As a synthetic intermediate, its quality is typically confirmed by analytical methods such as HPLC and NMR, with a standard purity of 95-98%. The molecular weight of PEG polymers is polydisperse, and the reported molecular weight (MW 1690) is an average value.
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| Cell Assay |
N/A; this linker is not tested alone in cell-based assays. It is used as a building block for constructing PROTACs. In a typical synthesis, the terminal carboxylic acid is activated with EDC and NHS and reacted with a primary amine-containing ligand (either a target protein ligand or an E3 ligase ligand). The resulting PROTAC conjugate is then tested in cells for target degradation activity.
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| Animal Protocol |
N/A; no animal studies are performed with the linker alone. For a complete PROTAC conjugate, in vivo studies are conducted following institutional guidelines to evaluate its pharmacokinetic properties and efficacy. The long PEG chain may enhance the circulation half-life and reduce immunogenicity of the PROTAC molecule. The compound is typically formulated in a vehicle containing DMSO, PEG300, Tween-80, and saline for intraperitoneal (IP) or intravenous (IV) administration.
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| ADME/Pharmacokinetics |
This compound has a molecular weight of 1690.00, a molecular formula of C76H152O39, and a standard purity of 95-98%. It appears as a solid powder at room temperature. For storage, it should be kept as a powder at -20degC, sealed, and away from moisture. In a solvent, it can be stored at -80degC for 6 months or at -20degC for 1 month, sealed, and away from moisture. It is soluble in DMSO and other organic solvents. The IUPAC name is 2,5,8,11,14,17,20,23,26,29,32,35,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98,101,104,107,110-pentatriacontaoxatridec-113-oic acid.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not intended for human therapeutic or clinical applications. Standard chemical safety precautions should be observed during handling. The product is stable under recommended storage conditions. For long-term storage, it should be kept as a powder at -20degC, away from moisture and light. This compound is not an approved drug and has not been cleared for clinical use.
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| References | |
| Additional Infomation |
The extremely long PEG37 spacer (37 ethylene glycol units) provides exceptional water solubility and flexibility, which is particularly useful for constructing PROTACs targeting large proteins or proteins with complex binding interfaces. The terminal carboxylic acid group enables versatile conjugation strategies, making this linker a valuable building block for PROTAC libraries, antibody-drug conjugates, and PEGylation of therapeutic proteins. This compound is also known as mPEG37-propionic acid and is valued for its versatility, biocompatibility, and ability to improve the pharmacokinetic properties of conjugated therapeutics.
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| Molecular Formula |
C76H152O39
|
|---|---|
| Molecular Weight |
1690.00
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| Exact Mass |
1688.991
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| CAS # |
2924199-92-6
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| PubChem CID |
77078315
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
39
|
| Rotatable Bond Count |
111
|
| Heavy Atom Count |
115
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| Complexity |
1520
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(=O)O
|
| InChi Key |
RWUISXIJAOBWHW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C76H152O39/c1-79-4-5-81-8-9-83-12-13-85-16-17-87-20-21-89-24-25-91-28-29-93-32-33-95-36-37-97-40-41-99-44-45-101-48-49-103-52-53-105-56-57-107-60-61-109-64-65-111-68-69-113-72-73-115-75-74-114-71-70-112-67-66-110-63-62-108-59-58-106-55-54-104-51-50-102-47-46-100-43-42-98-39-38-96-35-34-94-31-30-92-27-26-90-23-22-88-19-18-86-15-14-84-11-10-82-7-6-80-3-2-76(77)78/h2-75H2,1H3,(H,77,78)
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| Chemical Name |
3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[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]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoic acid
|
| 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 | 0.5917 mL | 2.9586 mL | 5.9172 mL | |
| 5 mM | 0.1183 mL | 0.5917 mL | 1.1834 mL | |
| 10 mM | 0.0592 mL | 0.2959 mL | 0.5917 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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