| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PEGs
As a linker, Bis-PEG10-t-butyl ester does not have a specific biological target. Instead, it serves as a chemical scaffold to connect two active ligands in the synthesis of PROTACs (Proteolysis Targeting Chimeras). One end is designed to bind an E3 ubiquitin ligase, and the other a target protein. By optimizing the distance and hydrophilicity between these ligands, the linker facilitates the formation of a ternary complex leading to targeted protein degradation. |
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| ln Vitro |
A linker separates the two ligands that make up PROTACs; one ligand is for an E3 ubiquitin ligase, and the other is for the target protein. Target proteins are selectively degraded by PROTACs by taking advantage of the intracellular ubiquitin-proteasome system[1].
Bis-PEG10-t-butyl ester is not used to assess biological activity in vitro as it is a chemical linker. However, when incorporated into a PROTAC molecule, the resulting conjugate demonstrates potent in vitro degradation activity against the intended target protein. For example, PROTACs built with PEG-based linkers (like PEG10) have shown high degradation efficacy (e.g., DC50 in the low nM range) and enhanced cellular permeability compared to other linker types. |
| ln Vivo |
Bis-PEG10-t-butyl ester is not used directly to study biological efficacy in vivo. Its role is within the final drug conjugate. PROTACs synthesized using PEG-based linkers like Bis-PEG10-t-butyl ester have demonstrated superior in vivo efficacy in mouse xenograft models. By improving water solubility and reducing immunogenicity, the PEG10 linker can help achieve higher oral bioavailability and better tumor exposure, leading to effective tumor growth inhibition.
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| Enzyme Assay |
In biochemical conjugation and PROTAC synthesis, this compound is used in a standard amide coupling reaction with amine-containing molecules in the presence of a coupling reagent like HATU or EDCI. The t-butyl ester protecting group is removed with TFA to reveal a free carboxylic acid for conjugation. The purity of the reaction products can be analyzed and confirmed by HPLC and LC-MS.
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| Cell Assay |
Bis-PEG10-t-butyl ester is not used in direct cellular experiments. As a building block, it is employed in the synthesis of PROTACs, which are then assessed in cellular assays. Cells are treated with a PROTAC synthesized from this linker for 4-24 hours. Target protein degradation is then evaluated by Western blot. These cellular assays help determine the DC50 (half-maximal degradation concentration) and Dmax (maximal degradation).
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| Animal Protocol |
There are no direct in vivo animal protocols for Bis-PEG10-t-butyl ester. However, for PROTACs synthesized using this linker, typical animal protocols involve pharmacokinetic (PK) studies and xenograft mouse models. To measure PD, after the final dose, tumors are excised and lysed, and the levels of the target protein are measured by Western blot to determine in vivo degradation efficacy.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic (PK) data for the linker itself are not applicable. The linker is a component that directly influences the PK properties of the final PROTAC conjugate. PEG10 is a hydrophilic and flexible spacer that generally improves water solubility, reduces aggregation, and can prolong the in vivo half-life of a drug conjugate by reducing its clearance. The primary function of the t-butyl ester is to protect the carboxylic acid during synthesis.
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| Toxicity/Toxicokinetics |
Toxicological data for the isolated linker are not applicable, as it is not administered as a therapeutic agent. The potential toxicity is attributed to the final PROTAC molecule. For the final PROTAC conjugate, toxicological assessments would include standard in vitro safety panels (e.g., hERG, CYP inhibition) and in vivo tolerability studies to identify the maximum tolerated dose in rodents.
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| References | |
| Additional Infomation |
Bis-PEG10-t-butyl ester (CAS: N/A) has a molecular formula of C32H62O14 and a molecular weight of 670.8 g/mol. It is a prototypical PROTAC linker. Its PEG10 spacer consists of ten ethylene glycol units, providing optimal solubility for bioconjugation. The compound is typically stored at -20degC. It is for research use only as a laboratory chemical for the synthesis of PROTACs and other conjugates.
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| Molecular Formula |
C32H62O14
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| Molecular Weight |
670.83
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| Appearance |
Colorless to light yellow liquid
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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 |
| 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 | 1.4907 mL | 7.4535 mL | 14.9069 mL | |
| 5 mM | 0.2981 mL | 1.4907 mL | 2.9814 mL | |
| 10 mM | 0.1491 mL | 0.7453 mL | 1.4907 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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