| 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, Amino-PEG24-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 two orthogonal functional groups (NH2 and COOH) enable sequential conjugation to two different ligands without the need for protecting groups. The extremely long PEG24 chain (24 ethylene glycol units) provides outstanding water solubility and flexibility, which can significantly improve the aqueous solubility, reduce aggregation, and extend the circulation half-life of the final PROTAC molecule. The terminal primary amine can be used for direct amide bond formation with a carboxylic acid-containing ligand using EDC/NHS, while the terminal carboxylic acid can be activated similarly for conjugation to an amine-containing ligand. |
| 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%. The molecular weight of PEG polymers is polydisperse, and the reported molecular weight (MW 1146.35) is an average value. The long PEG24 chain may complicate characterization, but the structure can be confirmed by NMR and mass spectrometry.
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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 carboxylic acid group is activated with EDC and NHS and reacted with a primary amine-containing ligand (e.g., an E3 ligase ligand). After deprotection of the amine (if necessary), the free primary amine is reacted with a carboxylic acid-containing ligand to form a second amide bond. The resulting PROTAC is then tested in cells for target degradation activity. The long PEG24 spacer is expected to significantly improve the cellular permeability and solubility of the final PROTAC molecule.
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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 PEG24 chain is expected to significantly prolong the circulation half-life and reduce immunogenicity of the PROTAC molecule compared to shorter PEG or alkyl linkers. 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 1146.35-1146.37, a molecular formula of C51H103NO26, and a standard purity of ≥95%. It appears as a solid powder. For storage, it should be kept as a powder at -20degC for up to 3 years or in a solvent at -80degC for 6 months. It is soluble in DMSO and other organic solvents. The product should be protected from light during storage. The IUPAC name is 1-amino-3,6,9,12,15,18,21,24,27,30,33,36,39,42,45,48,51,54,57,60,63,66,69,72-tetracosaoxapentapentacontan-75-oic acid.
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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 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. It is not an approved therapeutic drug and has not been cleared for clinical use.
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| References | |
| Additional Infomation |
The exceptionally long PEG24 spacer provides an extreme degree of water solubility and flexibility, making this linker ideal for constructing PROTACs targeting large protein complexes or proteins with binding sites that are far apart. The orthogonal functional groups (NH2 and COOH) enable sequential conjugation to two different ligands without protecting groups, simplifying the synthesis of heterobifunctional PROTACs. This linker is also widely used in bioconjugation, drug delivery systems, PEGylation of therapeutic proteins, and surface functionalization. The long PEG chain can effectively shield the conjugated molecule from immune recognition and reduce renal clearance, potentially improving the in vivo efficacy of the final conjugate.
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| Molecular Formula |
C51H103NO26
|
|---|---|
| Molecular Weight |
1146.3546
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| Exact Mass |
1145.676
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| CAS # |
2563873-76-5
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| PubChem CID |
51340925
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| Appearance |
White to off-white solid powder
|
| LogP |
-7
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
27
|
| Rotatable Bond Count |
74
|
| Heavy Atom Count |
78
|
| Complexity |
1080
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCN)C(=O)O
|
| InChi Key |
MNGHAJYOUCOMLD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C51H103NO26/c52-2-4-56-6-8-58-10-12-60-14-16-62-18-20-64-22-24-66-26-28-68-30-32-70-34-36-72-38-40-74-42-44-76-46-48-78-50-49-77-47-45-75-43-41-73-39-37-71-35-33-69-31-29-67-27-25-65-23-21-63-19-17-61-15-13-59-11-9-57-7-5-55-3-1-51(53)54/h1-50,52H2,(H,53,54)
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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-aminoethoxy)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 | 0.8723 mL | 4.3616 mL | 8.7233 mL | |
| 5 mM | 0.1745 mL | 0.8723 mL | 1.7447 mL | |
| 10 mM | 0.0872 mL | 0.4362 mL | 0.8723 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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