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| Other Sizes |
| Targets |
m-PEG2-amine does not target a biological receptor. Its function is as a chemical linker. The terminal primary amine (-NH₂) is the key reactive moiety. It reacts with carboxylic acids in the presence of coupling agents (e.g., EDC, HOBt) to form stable amide bonds. It also reacts with activated esters, such as N-hydroxysuccinimide (NHS) esters, to form amide linkages. This reactivity makes it a versatile linker for bioconjugation. In ADCs and PROTACs, it serves to connect the targeting or functional moiety to the payload or ligand.
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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 chemical linker, m-PEG2-amine has no intrinsic biological activity. Its utility is derived from its chemical reactivity. The amine group can be used to conjugate the PEG chain to a wide variety of molecules, including antibodies, drugs, and ligands. The short PEG2 spacer provides a balance between hydrophilicity and compactness, which can be advantageous when a minimal spacer is desired. The compound is classified as a cleavable ADC linker, meaning it is designed to be cleaved under specific conditions (e.g., in the acidic environment of a lysosome) to release the payload. |
| ln Vivo |
No direct in vivo activity is attributed to m-PEG2-amine itself. Its role is as a component in larger therapeutic constructs. In ADCs, the PEG2 linker connects the antibody to the cytotoxic drug, helping to improve the drug's solubility and stability in circulation. In PROTACs, it connects the target protein ligand to the E3 ubiquitin ligase ligand.
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| Enzyme Assay |
For in vitro characterization, m-PEG2-amine is typically analyzed by NMR and HPLC to confirm its structure and purity. Purity is often >98%. The amine content can be quantified by titration or by derivatization with a reagent such as ninhydrin or fluorescamine. Its solubility in various solvents is determined.
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| Cell Assay |
Cell-based assays are not performed on m-PEG2-amine alone. As a linker, it is incorporated into larger constructs (ADCs or PROTACs) that are then evaluated in cell culture. For example, an ADC containing the m-PEG2-amine linker would be tested for its ability to bind to cancer cells, be internalized, and deliver a cytotoxic payload.
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| Animal Protocol |
In vivo studies with m-PEG2-amine are conducted using the final conjugate (ADC or PROTAC). These studies typically involve administering the conjugate to animal models to assess its pharmacokinetics, efficacy, and safety. The PEG2 spacer contributes to the overall performance of the conjugate.
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| ADME/Pharmacokinetics |
As a linker, m-PEG2-amine does not have independent pharmacokinetic (PK) properties. However, the PEG2 spacer can improve the aqueous solubility of the final conjugate, which may positively impact its PK.
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| Toxicity/Toxicokinetics |
The toxicology of m-PEG2-amine is not typically evaluated independently. PEG is generally considered to be biocompatible and non-toxic. The compound is a cleavable linker, and its degradation products are expected to be non-toxic.
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| References | |
| Additional Infomation |
m-PEG2-amine is a short, cleavable PEG linker used in the synthesis of ADCs and PROTACs. It has a molecular weight of 119.16 g/mol and features a primary amine group for conjugation. The short PEG2 spacer improves aqueous solubility and is a valuable tool for drug delivery research, available for research use only.
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| Molecular Formula |
C5H13NO2
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|---|---|
| Molecular Weight |
119.16222
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| Exact Mass |
119.094
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| CAS # |
31576-51-9
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| Related CAS # |
80506-64-5
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| PubChem CID |
520530
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| Appearance |
Colorless to yellow liquid
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| Density |
0.9±0.1 g/cm3
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| Boiling Point |
163.7±15.0 °C at 760 mmHg
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| Flash Point |
54.1±27.7 °C
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| Vapour Pressure |
2.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.420
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| LogP |
-1.01
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
8
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| Complexity |
41.4
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COCCOCCN
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| InChi Key |
QWCGXANSAOXRFE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H13NO2/c1-7-4-5-8-3-2-6/h2-6H2,1H3
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| Chemical Name |
2-(2-methoxyethoxy)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 | 8.3921 mL | 41.9604 mL | 83.9208 mL | |
| 5 mM | 1.6784 mL | 8.3921 mL | 16.7842 mL | |
| 10 mM | 0.8392 mL | 4.1960 mL | 8.3921 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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