| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
As a linker, Amino-PEG8-acid does not have a traditional biological target. It is a chemical tool used in the synthesis of ADCs and PROTACs. Its role is to connect two functional molecules. The amino and carboxylic acid groups provide handles for conjugation. The long PEG8 spacer provides significant hydrophilicity and flexibility, which can improve the solubility and pharmacokinetic properties of the final conjugate.
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|---|---|
| ln Vitro |
ADC is made up of an antibody and an ADC linker that connects the ADC cytotoxin [1]. The target protein and the E3 ubiquitin ligase ligand are the two distinct ligands that make up PROTAC. They are joined by a linker. PROTAC degrades the target protein's quality by means of the intracellular ubiquitin-carotene body system [2].
In vitro, Amino-PEG8-acid is used as a linker in the synthesis of ADCs and PROTACs. Its utility is demonstrated by the successful creation of these bioconjugates. The long PEG8 spacer helps to mask hydrophobic payloads, reducing aggregation and improving the overall aqueous solubility of the conjugate. The non-cleavable nature provides stability in circulation. |
| ln Vivo |
In vivo applications of Amino-PEG8-acid are realized through the ADCs or PROTACs it helps construct. The long PEG8 spacer can significantly improve the pharmacokinetic properties of the conjugate by increasing its hydrodynamic volume, reducing renal clearance, and minimizing immunogenicity. The compound is a research tool for developing biopharmaceuticals with improved drug-like properties.
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| Enzyme Assay |
In vitro assays for Amino-PEG8-acid typically involve confirming its structure and purity by NMR and mass spectrometry. Its reactivity, such as amide bond formation, can be demonstrated by synthesizing a small molecule conjugate. The formation of the amide bond can be confirmed by HPLC or mass spectrometry. These protocols are for research purposes only.
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| Cell Assay |
In vitro cell-based assays for Amino-PEG8-acid are performed on the final conjugate, not the linker alone. For ADCs, cytotoxicity is measured using cell viability assays on target antigen-expressing cells. For PROTACs, target protein degradation is assessed by Western blot. The linker's contribution to the conjugate's solubility and cell permeability can be evaluated. Standard cell culture conditions are used.
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| Animal Protocol |
In vivo animal studies for Amino-PEG8-acid are conducted with the final conjugate. Xenograft mouse models are used to evaluate antitumor efficacy for ADCs or PROTACs targeting cancer proteins. The conjugate is administered intravenously. Tumor growth inhibition is monitored, and pharmacodynamic studies assess target engagement or degradation. Pharmacokinetic studies evaluate the conjugate's half-life and distribution. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Amino-PEG8-acid are not characterized independently. However, the long PEG8 spacer is known to significantly improve the pharmacokinetic profile of conjugates by increasing their half-life and reducing immunogenicity. The compound is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of Amino-PEG8-acid is evaluated as part of the final conjugate. The linker itself is designed to be non-toxic and biocompatible. The toxicity of the conjugate is primarily determined by the payload and the target. The compound is a research chemical, and its safety for human use has not been established.
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| References | |
| Additional Infomation |
Additional information: Amino-PEG8-acid has the CAS number 756526-04-2. Its molecular formula is C₁₉H₃₉NO₁₀. It is a non-cleavable ADC linker and a PROTAC linker. It contains an amino group and a terminal carboxylic acid. This product is for research use only and is not approved for clinical or therapeutic applications.
|
| Molecular Formula |
C19H39NO10
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|---|---|
| Molecular Weight |
441.513667345047
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| Exact Mass |
441.257
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| CAS # |
756526-04-2
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| PubChem CID |
51340929
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| Appearance |
White to light yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
547.1±50.0 °C at 760 mmHg
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| Flash Point |
284.7±30.1 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.470
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| LogP |
-3.36
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
30
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| Complexity |
349
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YLKOHZCQTVYVDB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H39NO10/c20-2-4-24-6-8-26-10-12-28-14-16-30-18-17-29-15-13-27-11-9-25-7-5-23-3-1-19(21)22/h1-18,20H2,(H,21,22)
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| Chemical Name |
3-[2-[2-[2-[2-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoic 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 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) |
DMSO : ~50 mg/mL (~113.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2650 mL | 11.3248 mL | 22.6495 mL | |
| 5 mM | 0.4530 mL | 2.2650 mL | 4.5299 mL | |
| 10 mM | 0.2265 mL | 1.1325 mL | 2.2650 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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