| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Bis-PEG2-NHS ester does not have a specific biological target, as it is a chemical linker rather than a pharmacologically active compound. Its function is purely structural, serving as a covalent connector between two or more molecular components. The "targets" of this linker are the primary amine groups (-NH2) on biomolecules, such as the lysine residues of proteins or the amino groups of peptides or other amine-containing molecules. The NHS ester groups react with primary amines to form stable amide bonds, releasing N-hydroxysuccinimide as a byproduct. This reaction is efficient and specific under mild conditions, making it a widely used method for bioconjugation. The PEG2 spacer is not a target but a structural element that enhances solubility and reduces steric hindrance between the conjugated molecules.
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| ln Vitro |
As a chemical linker, Bis-PEG2-NHS ester does not possess any direct in vitro biological activity, such as enzyme inhibition, receptor binding, or cytotoxicity. Its function is to serve as a covalent bridge in the synthesis of bioactive conjugates. The in vitro activity of this linker is assessed indirectly through the characterization of the final conjugates it helps to create. For instance, when used to synthesize an ADC, the activity of the conjugate is evaluated in cell-based assays for target binding, internalization, and cytotoxicity. The PEG2 linker contributes to the conjugate's overall activity by enhancing its solubility and providing the necessary spacing between the conjugated components. Thus, the activity of Bis-PEG2-NHS ester is a measure of its utility as a synthetic building block.
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| ln Vivo |
As a chemical linker, Bis-PEG2-NHS ester does not possess any direct in vivo biological activity. It is not administered as a therapeutic agent and does not exert pharmacological effects in animal models. Its in vivo relevance is strictly as a component of larger, biologically active conjugates. When incorporated into an ADC, the PEG2 linker contributes to the overall in vivo behavior of the conjugate. The hydrophilic PEG spacer is known to improve the pharmacokinetic profile of bioconjugates by increasing their solubility, reducing aggregation, and shielding them from immune recognition, thereby extending their circulation half-life. However, the specific in vivo activity—such as tumor regression—is determined by the conjugate's warhead and targeting ligand, not the linker itself. The linker's role is permissive, ensuring that the active components are stably connected and function optimally.
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| Enzyme Assay |
There are no specific in vitro enzyme or receptor binding assays for Bis-PEG2-NHS ester, as it is not a biologically active compound that directly interacts with proteins. The compound is a chemical reagent, and its characterization is performed using analytical chemistry techniques. The quality and identity of the linker are typically confirmed by methods such as Nuclear Magnetic Resonance (NMR) spectroscopy, High-Performance Liquid Chromatography (HPLC), and Mass Spectrometry (MS) to verify its structure and purity. The reactivity of the NHS ester groups can be tested by reacting the compound with a model amine (e.g., butylamine) and monitoring the formation of the amide bond by HPLC or LC-MS. This is a quality control step to ensure the linker is functional. There are no biological assays for this compound.
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| Cell Assay |
There are no standard in vitro cell-based assays for Bis-PEG2-NHS ester, as it is not a bioactive molecule intended to affect cellular function. Its use in cell biology is indirect, as a reagent for modifying other molecules. For example, it can be used to create ADCs or other bioconjugates that are then tested in cell-based assays. In such cases, the cell-based assay would involve treating cells with the final conjugated therapeutic and then measuring a biological readout, such as cell viability (for an ADC's cytotoxicity) or target engagement. The performance of the linker would be evaluated by the potency and selectivity of the conjugate, which depend on the linker's ability to connect the components effectively. However, there is no direct assay for the linker itself in cells, as it is not designed to interact with cells in its unconjugated form.
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| Animal Protocol |
Bis-PEG2-NHS ester is not used in in vivo animal experiments as a standalone compound, as it has no direct biological activity. It is a synthetic building block for creating ADCs and other bioconjugates. Animal studies involving this compound would only be conducted on the final, larger conjugates that incorporate it. In such studies, the linker's contribution to the overall pharmacokinetic and pharmacodynamic profile of the conjugate would be assessed. For example, researchers might compare the in vivo efficacy and half-life of an ADC synthesized with this PEG2 linker to one synthesized with a different linker. However, there is no standard animal protocol for the linker itself. Its use is limited to the research and development phase, where it is employed in the chemical synthesis of test articles.
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| ADME/Pharmacokinetics |
Bis-PEG2-NHS ester has a molecular weight of 400.34 g/mol and a molecular formula of C16H20N2O10. It is a white to off-white solid powder. The compound has a logP of -2.2, indicating high hydrophilicity. It is soluble in DMSO at ~100 mg/mL (~249.79 mM). For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound is stable at ambient temperature for a few days during shipping. Pharmacokinetic properties are not relevant as the compound is a linker, not a therapeutic agent.
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| Toxicity/Toxicokinetics |
Bis-PEG2-NHS ester is considered to have low toxicity, consistent with other PEG-based linkers. PEG polymers are widely regarded as biocompatible, non-toxic, and non-immunogenic. The compound is classified as a research reagent, and standard laboratory safety precautions should be followed when handling it. Its toxicity profile has not been extensively studied, but due to its intended use and chemical class, it is not expected to be acutely toxic. The compound is a non-cleavable linker, meaning it is designed to be stable and not degrade under physiological conditions. This stability is a desirable feature for its intended use, but it also means that if it were to enter the body as part of a conjugate, it would not be readily broken down.
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| Additional Infomation |
Bis-PEG2-NHS ester is a research-use-only reagent and is not a drug, nor is it approved for any clinical or therapeutic use. It is a homobifunctional PEG linker containing two NHS ester groups, used for crosslinking amine-containing biomolecules. The PEG2 spacer minimizes steric hindrance and improves aqueous solubility, supporting multivalent conjugation. Bis-PEG2-NHS ester is a non-degradable linker that may be utilized to prepare active antibody-drug conjugates (ADCs). Its mechanism of action is purely chemical: the NHS ester groups react with primary amines to form stable amide bonds. The compound is a valuable tool for bioconjugation, enabling the creation of stable, well-defined conjugates for research applications.
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| Molecular Formula |
C16H20N2O10
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| Molecular Weight |
400.3374
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| Exact Mass |
400.112
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| CAS # |
65869-63-8
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| Related CAS # |
123502-57-8
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| PubChem CID |
13055590
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| Appearance |
White to off-white solid powder
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| LogP |
-2.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
28
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| Complexity |
574
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SORMJGWNAXHOFC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H20N2O10/c19-11-1-2-12(20)17(11)27-15(23)5-7-25-9-10-26-8-6-16(24)28-18-13(21)3-4-14(18)22/h1-10H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[2-[3-(2,5-dioxopyrrolidin-1-yl)oxy-3-oxopropoxy]ethoxy]propanoate
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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) |
DMSO : ~100 mg/mL (~249.79 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.24 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 (6.24 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 (6.24 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 | 2.4979 mL | 12.4894 mL | 24.9788 mL | |
| 5 mM | 0.4996 mL | 2.4979 mL | 4.9958 mL | |
| 10 mM | 0.2498 mL | 1.2489 mL | 2.4979 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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