| Size | Price | |
|---|---|---|
| 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, Me-PEG4-Me itself has no intrinsic biological activity; it serves as a structural spacer in the synthesis of PROTAC molecules. The methyl end caps are inert and do not participate in conjugation reactions, making Me-PEG4-Me a non-reactive building block. In PROTAC synthesis, it is typically used as a flexible, hydrophilic segment within a larger linker structure. For example, a carboxylic acid or amine group can be introduced at one or both ends by converting the methyl groups to more reactive functional groups via chemical modification. Alternatively, Me-PEG4-Me is commonly used as a solvent, co-solvent, or plasticizer in PROTAC formulation and synthesis due to its excellent solubility properties and low viscosity. |
| 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.
|
| Enzyme Assay |
N/A; this compound is not assessed in isolated enzyme/receptor binding assays. As a synthetic intermediate or solvent, its quality is typically confirmed by analytical methods such as HPLC and GC, with a standard purity of ≥98%. The methyl groups can be characterized by their characteristic chemical shifts in NMR spectroscopy. The compound is often used as a reference standard in analytical chemistry.
|
| Cell Assay |
N/A; this linker is not tested alone in cell-based assays. It is used as a building block for constructing PROTACs or as a solvent in PROTAC synthesis. In a typical PROTAC synthesis, Me-PEG4-Me can be used as a starting material for the introduction of terminal functional groups. For example, one or both methyl groups can be converted to carboxylic acids via oxidation, or to amines via substitution reactions. The resulting functionalized PEG4 linker can then be used in standard amide coupling reactions to attach target protein ligands and E3 ligase ligands. The resulting PROTAC is then tested in cells for target degradation activity.
|
| 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. The compound is typically formulated using a vehicle containing DMSO, PEG300, Tween-80, and saline and administered via intraperitoneal (IP) or intravenous (IV) injection. The PEG4 spacer may improve the pharmacokinetic properties of the conjugate by enhancing water solubility and reducing aggregation.
|
| ADME/Pharmacokinetics |
This compound has a molecular weight of 222.28, a molecular formula of C10H22O5, and a standard purity of ≥98%. It appears as a colorless liquid. The IUPAC name is 2,5,8,11,14-pentaoxapentadecane. For storage, it should be kept as a liquid at 4degC for up to 2-3 years, sealed, away from moisture. It is soluble in DMSO, ethanol, and other organic solvents. The product is also miscible with water. Density is approximately 1.013 g/mL at 25degC. It is also known as tetraglyme or tetraethylene glycol dimethyl ether. CAS: 143-24-8.
|
| Toxicity/Toxicokinetics |
This product is for research use only and is not for human therapeutic or clinical applications. Standard chemical safety precautions should be observed during handling. The product is stable under recommended storage conditions. It is not an approved therapeutic drug and has not been cleared for clinical use. It is a PROTAC linker and laboratory solvent used for research and development purposes only.
|
| 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 |
Tetraethylene glycol dimethyl ether is a polyether.
Me-PEG4-Me (tetraglyme) is a widely used solvent in organic synthesis and electrochemistry due to its high thermal stability and ability to dissolve a wide range of organic and inorganic compounds. In PROTAC research, it serves as a flexible, hydrophilic PEG4 building block that can be functionalized at the termini for conjugation to ligands. Its symmetric, non-reactive nature makes it an ideal starting material for the synthesis of heterobifunctional PEG4 linkers, as only one methyl group can be selectively oxidized or modified to introduce an orthogonal functional group. This compound is also known as tetraethylene glycol dimethyl ether and is a valuable reagent for PEGylation and linker chemistry. |
| Molecular Formula |
C10H22O5
|
|---|---|
| Molecular Weight |
222.28
|
| Exact Mass |
222.146
|
| CAS # |
143-24-8
|
| PubChem CID |
8925
|
| Appearance |
Colorless to light yellow liquid（Density：1.009 g/cm3）
|
| Density |
1.0±0.1 g/cm3
|
| Boiling Point |
275.3±0.0 °C at 760 mmHg
|
| Melting Point |
−30 °C(lit.)
|
| Flash Point |
140.6±0.0 °C
|
| Vapour Pressure |
0.0±0.5 mmHg at 25°C
|
| Index of Refraction |
1.421
|
| LogP |
-1.51
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
15
|
| Complexity |
98
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COCCOCCOCCOCCOC
|
| InChi Key |
ZUHZGEOKBKGPSW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H22O5/c1-11-3-5-13-7-9-15-10-8-14-6-4-12-2/h3-10H2,1-2H3
|
| Chemical Name |
1-methoxy-2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethane
|
| HS Tariff Code |
2934.99.9001
|
| 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, 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)
|
| Solubility (In Vitro) |
H2O :≥ 100 mg/mL (~449.88 mM)
|
|---|---|
| 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 | 4.4988 mL | 22.4942 mL | 44.9883 mL | |
| 5 mM | 0.8998 mL | 4.4988 mL | 8.9977 mL | |
| 10 mM | 0.4499 mL | 2.2494 mL | 4.4988 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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