| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Propargyl-PEG3-acid is a linker molecule and does not possess a specific biological target or receptor. Its "target" is the functional groups it reacts with: primary amines (via the carboxylic acid group after activation with EDC or HATU) and organic azides (via the alkyne group in a copper-catalyzed azide-alkyne cycloaddition). In the context of drug conjugate synthesis, it serves as a non-cleavable bridge connecting a targeting moiety (e.g., antibody) to a payload (e.g., cytotoxin) or an E3 ligase ligand. Its role is purely chemical, providing the required spatial arrangement and stability without interfering with biological recognition.
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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.
Propargyl-PEG3-acid does not exhibit intrinsic pharmacological activity in vitro; its activity is defined by its chemical reactivity and utility as a building block. It is used to synthesize 6-OHDA-PEG3-yne, a neurotoxin conjugate, demonstrating its versatility. Its high purity and defined PEG chain length ensure reproducible conjugation efficiency in biochemical assays. The PEG3 spacer enhances the water solubility of conjugated molecules, which is critical for maintaining their activity in aqueous biological buffers. It is also employed in the preparation of multifunctional nanoparticles and surface coatings for biosensors. |
| ln Vivo |
Specific in vivo activity data for Propargyl-PEG3-acid itself is not applicable, as it is not a therapeutic agent. However, the conjugates synthesized using this linker, such as PROTACs or ADC candidates, are designed for in vivo efficacy. The linker's stability, solubility, and clearance properties directly influence the pharmacokinetics of the final construct. For example, PEG3 linkers often confer prolonged circulation time and reduced immunogenicity. In animal models, the efficacy of the conjugated drug is evaluated, and the linker's contribution to the overall therapeutic index is assessed through comparative studies with other linker chemistries.
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| Enzyme Assay |
The reactivity of Propargyl-PEG3-acid is assessed in cell-free chemical conjugation assays. For the carboxylic acid, its ability to form an amide bond is tested by reacting it with a model primary amine (e.g., benzylamine) in the presence of a coupling reagent like EDC or HATU. The reaction yield is monitored by TLC, HPLC, or LC-MS. For the alkyne, its click reactivity is evaluated by reacting with a model azide (e.g., benzyl azide) under CuAAC conditions. The formation of the triazole product is confirmed by mass spectrometry and NMR. These assays ensure the functional integrity of the linker before use in complex bioconjugation.
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| Cell Assay |
In cellular assays, Propargyl-PEG3-acid is not used directly as a modulator; rather, it is a component for synthesizing cell-permeable probes or drug conjugates. For example, a fluorescent azide can be clicked onto a cell-surface glycoprotein labeled with an alkyne via this linker, enabling live-cell imaging. Alternatively, it is used to synthesize PROTACs that are then tested for target protein degradation in cancer cell lines. The linker’s contribution to cellular uptake and intracellular stability is evaluated by comparing the activity of conjugates with different PEG lengths or different linker types.
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| Animal Protocol |
Propargyl-PEG3-acid is not administered in animal studies as a standalone compound. It is integral to the synthesis of drug conjugates that are subsequently tested in vivo. For instance, an ADC synthesized using this linker is dosed in xenograft mouse models to assess tumor growth inhibition. The linker’s susceptibility to enzymatic cleavage, its effect on plasma half-life, and its influence on off-target toxicity are evaluated through pharmacokinetic and toxicokinetic analyses. In such studies, the linker’s performance is benchmarked against cleavable or more hydrophilic linkers to optimize the therapeutic window.
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| ADME/Pharmacokinetics |
Propargyl-PEG3-acid is a small hydrophilic molecule with a calculated LogP of -0.72, indicating good aqueous solubility. It is typically stored as a solid at -20°C and is stable for up to 2 years. When dissolved in DMSO or water, it should be used immediately to avoid hydrolysis of the acid group. Its pharmacokinetic properties are not directly measured, but PEG3 linkers generally confer enhanced solubility and reduced aggregation, which can improve the overall PK profile of large biomolecule conjugates. The acid group allows for easy radiolabeling or fluorescent tagging for tracking purposes.
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| Toxicity/Toxicokinetics |
Propargyl-PEG3-acid is considered low toxicity as a chemical reagent. However, standard laboratory safety precautions should be observed, including wearing gloves and eye protection. It is not known to be mutagenic or carcinogenic. In the context of drug conjugates, the safety profile is determined by the payload and targeting moiety, not the linker itself. PEG-based linkers are generally regarded as safe and biocompatible, with limited immunogenicity. Detailed toxicological data is not available because it is not a pharmaceutical active ingredient; its use is restricted to research and development.
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| References |
[1]. Farzam A, et al. A functionalized hydroxydopamine quinone links thiol modification to neuronal cell death. Redox Biol. 2020 Jan;28:101377.
[2]. Albone, Earl F, et al. ERIBULIN-BASED ANTIBODY-DRUG CONJUGATES AND METHODS OF USE. Patent. 20170252458. |
| Additional Infomation |
Propargyl-PEG3-acid is a commercially available research-grade linker, widely used in academia and industry for the synthesis of bioconjugates, drug delivery systems, and diagnostic probes. Its well-defined PEG3 structure ensures batch-to-batch consistency, which is critical for reproducible biological studies. It is not an FDA-approved drug and is not intended for human use. It is a key reagent in the development of next-generation targeted therapies, including antibody-drug conjugates and proteolysis-targeting chimeras. Its adoption has grown with the rise of click chemistry and precision medicine approaches.
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| Molecular Formula |
C10H16O5
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|---|---|
| Molecular Weight |
216.233
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| Exact Mass |
216.099
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| CAS # |
1347760-82-0
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| PubChem CID |
60146217
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| Appearance |
Colorless to light yellow liquid（Density：1.131±0.06 g/cm3）
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
348.0±32.0 °C at 760 mmHg
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| Flash Point |
131.8±18.6 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.467
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| LogP |
-0.44
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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 |
10
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| Heavy Atom Count |
15
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| Complexity |
205
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCC#C)CCOCCC(=O)O
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| InChi Key |
CJNSWLAJTZVSRB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H16O5/c1-2-4-13-6-8-15-9-7-14-5-3-10(11)12/h1H,3-9H2,(H,11,12)
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| Chemical Name |
3-[2-(2-prop-2-ynoxyethoxy)ethoxy]propanoic acid
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| Synonyms |
Propyne-PEG2-CH2CH2COOH; Propargyl-PEG3-acid
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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 | 4.6247 mL | 23.1235 mL | 46.2471 mL | |
| 5 mM | 0.9249 mL | 4.6247 mL | 9.2494 mL | |
| 10 mM | 0.4625 mL | 2.3124 mL | 4.6247 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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