| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
As a PEG-based linker rather than a pharmacologically active drug, Amino-PEG8-t-butyl ester does not possess a defined biological target or receptor. Its role in biochemical applications is to serve as a structural spacer and conjugation bridge between bioactive molecules, such as antibodies and cytotoxic payloads in ADCs, or between an E3 ubiquitin ligase ligand and a target protein ligand in PROTACs. The amino group is reactive with electrophilic targets, forming stable covalent bonds, while the t-butyl ester provides a protected handle for orthogonal deprotection and functionalization.
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| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC. Two distinct ligands, one for the E3 ubiquitin ligase and the other for the target protein, are present in PROTAC and are joined by a linker. PROTAC targets and selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system.
In vitro, Amino-PEG8-t-butyl ester functions as a cleavable ADC linker that enables the attachment of cytotoxic agents to monoclonal antibodies. ADCs consist of an antibody linked to an ADC cytotoxin via an ADC linker. In PROTAC applications, the PEG linker connects a ligand for an E3 ubiquitin ligase to a ligand for the target protein, allowing the PROTAC to exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. The hydrophilic PEG spacer enhances aqueous solubility and reduces aggregation of conjugated biomolecules. |
| ln Vivo |
In vivo, Amino-PEG8-t-butyl ester is not a therapeutic agent itself but a chemical tool used in the construction of biopharmaceuticals. The resulting ADC or PROTAC conjugates incorporating this PEG linker are designed for in vivo administration to achieve targeted therapy or protein degradation. The PEG spacer helps improve the pharmacokinetic properties of the conjugate by increasing hydrodynamic volume, reducing renal clearance, and minimizing immunogenicity. The cleavable nature of the ester allows for controlled release of the payload under specific physiological conditions, enhancing therapeutic efficacy and reducing off-target toxicity.
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| Enzyme Assay |
For in vitro enzyme/receptor binding studies, Amino-PEG8-t-butyl ester is typically evaluated as part of an ADC or PROTAC construct rather than as a standalone compound. The linker’s ability to be cleaved by TFA can be verified by HPLC or mass spectrometry. Binding affinity of the complete ADC to its target antigen can be assessed using surface plasmon resonance (SPR) or enzyme-linked immunosorbent assay (ELISA). The efficiency of PROTAC-mediated ternary complex formation can be evaluated using AlphaScreen or bioluminescence resonance energy transfer (BRET) assays. These methods are for reference only and require independent validation.
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| Cell Assay |
In vitro cell-based assays for Amino-PEG8-t-butyl ester typically involve testing the biological activity of the complete ADC or PROTAC conjugate rather than the linker alone. For ADCs, cell viability assays (e.g., MTT or CellTiter-Glo) are performed on target antigen-expressing cancer cell lines to assess cytotoxicity. For PROTACs, cellular degradation assays using Western blot or quantitative mass spectrometry are conducted to measure target protein knockdown. The PEG linker’s contribution to solubility and cell permeability can be evaluated in these cellular systems. Standard cell culture conditions (37°C, 5% CO₂) are used with appropriate media and serum supplementation.
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| Animal Protocol |
In vivo animal studies using Amino-PEG8-t-butyl ester are conducted with the final ADC or PROTAC conjugate, not the linker alone. Typical protocols involve xenograft mouse models bearing human tumor cells to evaluate antitumor efficacy. For ADCs, dosing regimens (e.g., intravenous administration, 1-10 mg/kg, weekly or biweekly) are employed to assess tumor growth inhibition, survival benefit, and pharmacokinetics. For PROTACs, similar efficacy studies are performed along with pharmacodynamic assessments of target protein degradation in tumor tissues. Formulation preparation typically involves dissolving the compound in DMSO followed by dilution with PEG300, Tween 80, and saline or PBS.
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| ADME/Pharmacokinetics |
As a PEG linker rather than a drug, Amino-PEG8-t-butyl ester does not have intrinsic pharmacokinetic properties. However, PEG linkers in general contribute to the pharmacokinetic profile of ADCs and PROTACs by increasing hydrodynamic radius, reducing renal filtration, and prolonging circulation half-life. The hydrophilic PEG spacer minimizes opsonization and uptake by the reticuloendothelial system. The cleavable t-butyl ester allows for pH- or enzyme-triggered payload release. The pharmacokinetics of the final conjugate depend on multiple factors including the antibody, payload, and conjugation site, with typical ADC half-lives ranging from several days to weeks in preclinical species.
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| Toxicity/Toxicokinetics |
As a chemical linker not intended for direct therapeutic use, Amino-PEG8-t-butyl ester has limited toxicity data available. The compound is classified for research use only and not for human consumption. General safety precautions for handling PEG-based reagents apply, including the use of personal protective equipment and working in a fume hood. The final ADC or PROTAC conjugates incorporating this linker undergo extensive toxicological evaluation in preclinical species (e.g., rats and cynomolgus monkeys) to assess maximum tolerated dose, target organ toxicity, and off-target effects prior to clinical development.
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| References | |
| Additional Infomation |
Additional information: Amino-PEG8-t-butyl ester is also known as Amino-PEG8-Boc and has the molecular formula C₂₃H₄₇NO₁₀ with a molecular weight of 497.62 g/mol. The MDL number is MFCD11041142. This compound is part of a family of PEG linkers with varying ethylene glycol unit lengths (e.g., PEG4, PEG6, PEG12) that allow fine-tuning of solubility, flexibility, and pharmacokinetic properties of the final conjugate. The Boc-protected amine enables selective deprotection under acidic conditions for orthogonal conjugation strategies. This product is for research purposes only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C23H47NO10
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| Molecular Weight |
497.619988679886
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| Exact Mass |
497.32
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| CAS # |
756526-06-4
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| PubChem CID |
53433575
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| Appearance |
Colorless to light yellow liquid
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| LogP |
1.51
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
34
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(CCOCCOCCOCCOCCOCCOCCOCCOCCN)=O)C(C)(C)C
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| InChi Key |
UMJVFHNJPJVDSB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H47NO10/c1-23(2,3)34-22(25)4-6-26-8-10-28-12-14-30-16-18-32-20-21-33-19-17-31-15-13-29-11-9-27-7-5-24/h4-21,24H2,1-3H3
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| Chemical Name |
tert-butyl 3-[2-[2-[2-[2-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoate
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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 | 2.0096 mL | 10.0478 mL | 20.0957 mL | |
| 5 mM | 0.4019 mL | 2.0096 mL | 4.0191 mL | |
| 10 mM | 0.2010 mL | 1.0048 mL | 2.0096 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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