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| Targets |
As a chemical linker, m-PEG7-aldehyde 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. The aldehyde group enables site-selective oxime or hydrazone ligation with hydrazide or aminooxy groups. In PROTAC applications, the linker connects an E3 ubiquitin ligase ligand to a target protein ligand. The PEG7 spacer improves aqueous solubility and reduces aggregation of the final conjugates. This linker does not bind to biological receptors or enzymes.
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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.
As a synthetic linker molecule, m-PEG7-aldehyde 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 ADCs, cytotoxicity is assessed using cell viability assays. The compound is water-soluble. |
| ln Vivo |
No direct in vivo pharmacological activity is attributed to m-PEG7-aldehyde. 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 saline or buffer. 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 aldehyde group may form reversible Schiff bases with amines under physiological conditions.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to m-PEG7-aldehyde 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 and structural integrity is confirmed by ¹H NMR, ¹³C NMR, and mass spectrometry. The aldehyde group content is verified through spectroscopic analysis or titration. For researchers using this linker, oxime or hydrazone formation reactions are monitored by TLC, HPLC, or LC-MS. Solubility testing in various solvents is performed to guide formulation development.
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| Cell Assay |
Cell-based assays are not performed directly on m-PEG7-aldehyde 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). Cell viability, proliferation, and apoptosis are monitored using standard assays. The linker's contribution to the construct's cellular uptake, stability, and efficacy is inferred from comparative studies. DMSO or water 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-PEG7-aldehyde, 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. 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-PEG7-aldehyde 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 PEG7 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.
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| Toxicity/Toxicokinetics |
Standard laboratory safety precautions should be followed when handling m-PEG7-aldehyde: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability. Aldehydes may be sensitive to oxidation and should be handled under inert atmosphere if possible. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling.
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| References |
[1]. Erwin R. Boghaert, et al. Anti-egfr antibody drug conjugates. WO2017214282A1.
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| Additional Infomation |
Additional information for m-PEG7-aldehyde: The compound has a CAS number of 1058691-77-2. Its molecular weight is 352.42 g/mol. Synonyms include m-PEG6-CH2CH2CHO. It is a non-cleavable ADC linker and a PEG-based PROTAC linker. It is a water-soluble compound. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C16H32O8
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|---|---|
| Molecular Weight |
352.420486450195
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| Exact Mass |
352.209
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| CAS # |
1058691-77-2
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| PubChem CID |
102514883
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| Appearance |
Colorless to light yellow liquid（Density：1.1±0.1 g/cm3）
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
424.7±40.0 °C at 760 mmHg
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| Flash Point |
182.2±27.4 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.442
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| LogP |
-2.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
24
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| Complexity |
240
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOC)CCOCCOCCOCCC=O
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| InChi Key |
OFRPYQRIPDCCAA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H32O8/c1-18-5-6-20-9-10-22-13-14-24-16-15-23-12-11-21-8-7-19-4-2-3-17/h3H,2,4-16H2,1H3
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| Chemical Name |
3-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanal
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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 | 2.8375 mL | 14.1876 mL | 28.3752 mL | |
| 5 mM | 0.5675 mL | 2.8375 mL | 5.6750 mL | |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8375 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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