| Size | Price | Stock | Qty |
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| 1g |
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| Other Sizes |
| Targets |
As a chemical linker, m-PEG4-amine does not bind to biological targets. Its functional "targets" are the chemical groups on molecules to which it conjugates. In ADC applications, the linker attaches cytotoxic payloads to monoclonal antibodies through stable covalent bonds. The terminal amine group provides a handle for conjugation to carboxylic acids (via amide bond formation using EDC/HATU activation), activated NHS esters, or carbonyls (via reductive amination). In PROTAC applications, the linker connects an E3 ubiquitin ligase ligand to a target protein ligand. The PEG4 spacer improves aqueous solubility and biocompatibility. This linker does not bind to biological receptors or enzymes.
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| ln Vitro |
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. An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC.
As a synthetic linker molecule, m-PEG4-amine does not exhibit pharmacological activity in cell-based assays. Its in vitro utility is demonstrated through the successful synthesis and characterization of ADC or PROTAC constructs incorporating this linker. Researchers evaluate the linker's performance by assessing conjugation efficiency (via HPLC, LC-MS, or NMR), the stability of resulting conjugates in cell culture media, and the biological activity of final constructs in target cell lines. For PROTACs, target protein degradation is quantified by Western blot or ELISA. For ADCs, cytotoxicity is assessed using cell viability assays. The compound is soluble in DMSO (10 mM). |
| ln Vivo |
No direct in vivo pharmacological activity is attributed to m-PEG4-amine. Its in vivo relevance is demonstrated through the performance of ADC or PROTAC constructs synthesized using this linker in animal models. For in vivo administration, conjugates are typically formulated in vehicles such as DMSO/PEG300/Tween-80/saline. The linker's stability in biological matrices, its contribution to the construct's pharmacokinetic profile, and its ability to maintain construct integrity are key parameters evaluated in preclinical studies. The PEG4 spacer enhances aqueous solubility and may improve pharmacokinetic properties.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to m-PEG4-amine as it is a chemical linker with no intrinsic affinity for biological macromolecules. Quality control and characterization are performed using standard analytical methods. Purity is assessed by HPLC (≥97%) and structural integrity is confirmed by ¹H NMR, ¹³C NMR, and mass spectrometry. The amine group content is verified through spectroscopic analysis or titration. For researchers using this linker, conjugation reactions (e.g., amide bond formation) are monitored by TLC, HPLC, or LC-MS. Solubility testing in various solvents is performed to guide formulation development. The compound is soluble in DMSO (10 mM).
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| Cell Assay |
Cell-based assays are not performed directly on m-PEG4-amine because it is a synthetic linker lacking biological activity. However, the biological activity of ADC or PROTAC constructs containing this linker is evaluated in relevant cell lines. Typical protocols involve treating cells with the construct for 4-48 hours, then assessing target protein degradation (for PROTACs) or cytotoxicity (for ADCs) using standard assays. Cell viability, proliferation, and apoptosis are monitored using MTT, CCK-8, or flow cytometry. The linker's contribution to the construct's cellular uptake, stability, and efficacy is inferred from comparative studies. DMSO stock solutions are prepared and diluted in cell culture media.
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| Animal Protocol |
In vivo animal studies are conducted with ADC or PROTAC constructs incorporating m-PEG4-amine, not with the linker alone. Typical protocols utilize rodent models (e.g., mice bearing tumor xenografts). The construct is administered via intravenous, intraperitoneal, or other routes at doses determined by preliminary pharmacokinetic and tolerability studies. Efficacy is assessed by measuring disease progression endpoints such as tumor volume, biomarker levels, or survival. Pharmacodynamic endpoints include target protein degradation (for PROTACs) or tumor growth inhibition (for ADCs). The linker's stability in circulation is evaluated through plasma sampling and LC-MS/MS analysis.
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| ADME/Pharmacokinetics |
As a chemical linker, m-PEG4-amine does not have a conventional pharmacokinetic profile. However, the pharmacokinetic properties of bioconjugates incorporating this linker are evaluated in preclinical studies. Following administration in rodents, key parameters such as half-life, clearance, volume of distribution, and bioavailability are determined from plasma concentration-time data. The PEG4 spacer contributes to enhanced aqueous solubility, reduced protein binding, and potentially prolonged circulation time. Linker stability in plasma is assessed by measuring intact conjugate concentrations over time using LC-MS/MS. The compound itself is not administered systemically.
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| Toxicity/Toxicokinetics |
Standard laboratory safety precautions should be followed when handling m-PEG4-amine: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound is corrosive (Signal Word: Danger). It should be stored at 2-8°C. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. The compound is not classified as a hazardous drug but should be treated with care. Researchers should consult the safety data sheet (SDS) before handling and follow institutional chemical safety guidelines.
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| References |
[1]. Hervé Bouchard, et al. Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation. WO2018206635A1.
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| Additional Infomation |
Additional information for m-PEG4-amine: The compound has a CAS number of 85030-56-4. Its molecular formula is C₉H₂₁NO₄ and molecular weight is 207.27 g/mol. The IUPAC name is 2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethanamine. Synonyms include mPEG4-NH2, 3,6,9,12-Tetraoxatridecanamine. It is a versatile PEG linker for ADCs and PROTACs. Purity is typically ≥97%. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C9H21NO4
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| Molecular Weight |
207.2673
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| Exact Mass |
207.147
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| CAS # |
85030-56-4
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| PubChem CID |
22639371
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| Appearance |
Colorless to light yellow liquid（Density：1.005±0.06 g/cm3）
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| Density |
1.005 g/cm3
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| Boiling Point |
276.701ºC at 760 mmHg
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| Index of Refraction |
1.439
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| LogP |
0.341
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
14
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| Complexity |
103
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOCCN)C
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| InChi Key |
DQTQYVYXIOQYGN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H21NO4/c1-11-4-5-13-8-9-14-7-6-12-3-2-10/h2-10H2,1H3
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| Chemical Name |
2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethanamine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: ~200 mg/mL (~964.9 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (24.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (24.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 5 mg/mL (24.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8246 mL | 24.1231 mL | 48.2462 mL | |
| 5 mM | 0.9649 mL | 4.8246 mL | 9.6492 mL | |
| 10 mM | 0.4825 mL | 2.4123 mL | 4.8246 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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