| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Propargyl-PEG8-amine is a chemical linker that targets functional groups on biomolecules rather than biological receptors. Its propargyl (alkyne) group serves as a reaction partner for azide-containing compounds in CuAAC click chemistry reactions. The amine group reacts with carboxylic acids, activated NHS esters, and carbonyl groups, enabling covalent attachment to proteins, peptides, and other biomolecules. The PEG8 spacer provides hydrophilicity and flexibility, reducing aggregation and improving solubility in aqueous media. The compound is used as a non-cleavable ADC linker for antibody-drug conjugate synthesis.
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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.
In vitro, Propargyl-PEG8-amine is used as a chemical reagent in bioconjugation reactions rather than as a bioactive compound with intrinsic biological activity. The compound's alkyne group undergoes CuAAC reactions with azide-functionalized molecules, enabling the formation of stable triazole linkages. The amine group enables conjugation to carboxylate-containing molecules via amide bond formation using coupling reagents such as EDC or HATU, or to NHS ester-activated molecules. The PEG8 spacer imparts hydrophilicity to conjugates, improving their solubility and reducing non-specific interactions. |
| ln Vivo |
In vivo, Propargyl-PEG8-amine is not typically used as a therapeutic agent but rather as a linker component in the synthesis of drug conjugates and biomaterials. When incorporated into antibody-drug conjugates (ADCs) or other drug delivery systems, the PEG linker contributes to the pharmacokinetic properties of the conjugate. The hydrophilic PEG spacer reduces immunogenicity and extends circulation half-life by decreasing renal clearance and opsonization. The compound's in vivo behavior is determined by the specific conjugate in which it is incorporated rather than by the linker itself.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to Propargyl-PEG8-amine as it is a chemical linker rather than a bioactive compound targeting biological receptors. Instead, the compound is characterized by its chemical reactivity and suitability for bioconjugation. Quality control assays include HPLC analysis to determine purity, NMR spectroscopy to confirm structure, and functional assays to verify the reactivity of the alkyne and amine groups. The compound's solubility and stability in various solvents are also assessed to ensure compatibility with bioconjugation applications.
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| Cell Assay |
In vitro cellular assays are not typically performed with Propargyl-PEG8-amine alone, as it is used as a chemical reagent rather than a bioactive compound. However, when incorporated into antibody-drug conjugates or other targeted therapeutics, the resulting conjugates are evaluated in cell-based assays to assess target binding, internalization, and cytotoxicity. The PEG linker's contribution to conjugate properties is assessed by comparing conjugates with different linkers in terms of stability, solubility, and biological activity. Cell viability, proliferation, and receptor binding assays are used to characterize the final conjugate.
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| Animal Protocol |
In vivo animal experiments are not typically conducted with Propargyl-PEG8-amine alone. Instead, the compound is incorporated into antibody-drug conjugates or other drug delivery systems, and the resulting conjugates are evaluated in animal models. Pharmacokinetic studies assess the circulation half-life, tissue distribution, and clearance of the conjugate. Efficacy studies in tumor xenograft models evaluate the therapeutic activity of ADC conjugates containing Propargyl-PEG8-amine linkers. The PEG linker's contribution to in vivo performance is assessed by comparing conjugates with different linker compositions.
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| ADME/Pharmacokinetics |
Propargyl-PEG8-amine is a chemical linker rather than a drug substance, so traditional pharmacokinetic studies are not applicable. However, when incorporated into drug conjugates, the PEG linker influences the pharmacokinetics of the conjugate by providing hydrophilicity, reducing aggregation, and extending circulation half-life. The PEG8 spacer minimizes renal clearance and opsonization, resulting in prolonged exposure and improved delivery to target tissues. The linker's stability in biological fluids is an important factor in determining the overall pharmacokinetic profile of the conjugate.
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| Toxicity/Toxicokinetics |
Toxicity studies are not typically conducted with Propargyl-PEG8-amine alone, as it is used as a linker component rather than a therapeutic agent. However, the safety of PEG-based linkers is well-established, as PEG is generally recognized as safe and is widely used in pharmaceutical formulations. When incorporated into antibody-drug conjugates, the safety profile is determined by the entire conjugate, including the antibody, payload, and linker. Preclinical toxicology studies of ADC conjugates assess the safety of the complete molecule.
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| References | |
| Additional Infomation |
Propargyl-PEG8-amine is a heterobifunctional PEG linker used for click chemistry and bioconjugation applications. It contains an alkyne group for CuAAC reactions with azide-containing compounds and an amine group for conjugation to carboxylates, NHS esters, and carbonyls. The compound is used as a non-cleavable ADC linker in antibody-drug conjugate synthesis and as a PROTAC linker for the synthesis of PROTAC molecules. It is intended for research use only and is not approved for human therapeutic applications.
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| Molecular Formula |
C19H37NO8
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|---|---|
| Molecular Weight |
407.498986959457
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| Exact Mass |
407.251
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| CAS # |
1196732-52-1
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| Related CAS # |
1196732-52-1;
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| PubChem CID |
58078852
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| Appearance |
Colorless to light yellow liquid（Density：1.070±0.06 g/cm3）
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
477.4±40.0 °C at 760 mmHg
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| Flash Point |
232.8±21.0 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.466
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| LogP |
-2.61
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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 |
24
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| Heavy Atom Count |
28
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| Complexity |
337
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOCCN)CCOCCOCCOCCOCC#C
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| InChi Key |
HJYYOUVXTIUMEJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H37NO8/c1-2-4-21-6-8-23-10-12-25-14-16-27-18-19-28-17-15-26-13-11-24-9-7-22-5-3-20/h1H,3-20H2
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| Chemical Name |
2-[2-[2-[2-[2-[2-[2-(2-prop-2-ynoxyethoxy)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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 | 2.4540 mL | 12.2699 mL | 24.5399 mL | |
| 5 mM | 0.4908 mL | 2.4540 mL | 4.9080 mL | |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4540 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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