| Size | Price | |
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| Other Sizes |
| Targets |
m-PEG8-amine targets primary amine-reactive functional groups. The terminal amine reacts with carboxylic acids, NHS esters, isocyanates, and carbonyls to form stable bonds. In ADCs and PROTACs, it serves as a linker component. The PEG8 spacer provides excellent hydrophilicity and flexibility.
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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 chemical linker, m-PEG8-amine has no intrinsic pharmacological activity. Its utility is defined by its terminal amine reactivity. The PEG8 spacer provides excellent water solubility and reduces aggregation. The compound has a molecular weight of 383.48 and a density of 1.054 g/mL. |
| ln Vivo |
No direct in vivo activity is attributed to m-PEG8-amine. It functions as a linker in ADCs and PROTACs. The amine group enables conjugation to payload molecules. The PEG8 spacer improves solubility and reduces immunogenicity of the final conjugate.
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| Enzyme Assay |
For non-cell-based assays, m-PEG8-amine is characterized by NMR and HPLC (≥98% purity). The amine content can be quantified by titration or derivatization. Reactivity can be tested by reacting with a model NHS ester and monitoring by HPLC or LC-MS.
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| Cell Assay |
Cell-based assays are not performed on m-PEG8-amine alone. It is used to synthesize ADCs or PROTACs, which are then evaluated in cell culture. Standard protocols involve treating cancer cell lines with the conjugate at 0.001-10 µM for 24-72 hours.
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| Animal Protocol |
In vivo studies with m-PEG8-amine are conducted using the final ADC or PROTAC construct. Typical protocols involve administering the conjugate to tumor-bearing mouse models via intravenous injection at 1-10 mg/kg. The PEG8 spacer contributes to prolonged circulation and enhanced efficacy.
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| ADME/Pharmacokinetics |
As a linker, m-PEG8-amine does not have independent PK properties. The PEG8 spacer improves aqueous solubility and reduces clearance. The compound has a discrete spacer length of 26 atoms spanning approximately 29.7 Å. Storage at 2-8°C is recommended.
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| Toxicity/Toxicokinetics |
Toxicology data specific to m-PEG8-amine are limited. The amine group may be irritating; standard safety precautions apply. PEG derivatives are biocompatible.
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| References | |
| Additional Infomation |
m-PEG8-amine is a cleavable ADC linker and a PEG-based PROTAC linker. Synonyms include 3,6,9,12,15,18,21,24-octaoxapentacosan-1-amine. The primary amine functionality enables efficient coupling to activated carboxylic acids and NHS esters. No clinical trials exist.
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| Molecular Formula |
C17H37NO8
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|---|---|
| Molecular Weight |
383.47758
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| Exact Mass |
383.252
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| CAS # |
869718-81-0
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| PubChem CID |
51340963
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.054
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| Boiling Point |
448ºC at 760 mmHg
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| Flash Point |
213.9ºC
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| LogP |
0.408
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
26
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| Complexity |
249
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOCCOCCOCCOCCOCCN)C
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| InChi Key |
YXWBFPPGROXJLL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H37NO8/c1-19-4-5-21-8-9-23-12-13-25-16-17-26-15-14-24-11-10-22-7-6-20-3-2-18/h2-18H2,1H3
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| Chemical Name |
2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]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) |
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 | 2.6077 mL | 13.0385 mL | 26.0770 mL | |
| 5 mM | 0.5215 mL | 2.6077 mL | 5.2154 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6077 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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