| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
As an ADC linker, Mal-amido-PEG1-C2-NHS ester does not have a specific biological target itself but serves as a chemical bridge between antibodies and cytotoxic payloads in antibody-drug conjugates. The maleimide group targets free thiol groups (-SH) on cysteine residues of antibodies or other proteins through Michael addition. The NHS ester reacts with primary amines on proteins, peptides, or other amine-containing molecules. The PEG spacer provides solubility and flexibility, reducing steric hindrance between the conjugated components.
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| ln Vitro |
In vitro activity of Mal-amido-PEG1-C2-NHS ester is assessed by its ability to conjugate to target proteins or antibodies. The efficiency of conjugation is typically evaluated by SDS-PAGE, Western blot, or mass spectrometry to confirm the formation of stable conjugates. The linker's reactivity with primary amines and thiol groups can be quantified using spectrophotometric methods or HPLC. The stability of the resulting conjugates in physiological conditions is also assessed to ensure the linker maintains the integrity of the ADC construct.
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| ln Vivo |
In vivo studies for Mal-amido-PEG1-C2-NHS ester are typically conducted as part of ADC development, where the complete antibody-drug conjugate is evaluated rather than the linker alone. The linker's performance in vivo is assessed through pharmacokinetic studies of the ADC, evaluating its stability in circulation, tumor targeting efficiency, and therapeutic efficacy in xenograft models. The non-cleavable nature of this linker ensures that the drug remains attached to the antibody until the ADC is internalized and degraded in the target cell.
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| Enzyme Assay |
For NHS ester reactivity assays, a solution of the linker in DMSO or DMF is added to a solution of amine-containing protein or peptide in PBS buffer at pH 7.4-8.5. The reaction mixture is incubated at room temperature for 1-4 hours, and the extent of conjugation is monitored by MALDI-TOF mass spectrometry or SDS-PAGE. For maleimide-thiol conjugation, the linker is reacted with thiol-containing compounds in PBS at pH 6.5-7.5, and the reaction progress is monitored by Ellman's assay or HPLC.
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| Cell Assay |
For protein labeling experiments, target proteins are dissolved in PBS buffer at pH 7.4. Mal-amido-PEG1-C2-NHS ester is dissolved in anhydrous DMSO or DMF and added to the protein solution at a molar ratio of 5-20:1 (linker:protein). The reaction is incubated at room temperature for 2-4 hours with gentle shaking. Excess linker is removed by dialysis or size-exclusion chromatography. The labeled protein is analyzed by SDS-PAGE, mass spectrometry, or UV-Vis spectroscopy to confirm successful conjugation and determine the degree of labeling.
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| Animal Protocol |
For ADC efficacy studies, immunocompetent or immunodeficient mice bearing human tumor xenografts are administered the complete ADC (containing Mal-amido-PEG1-C2-NHS ester as the linker) via intravenous injection. Dosing schedules typically involve multiple administrations at 1-2 week intervals. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity assessment. At study termination, tumors and major organs are collected for histopathological analysis and drug concentration measurement.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Mal-amido-PEG1-C2-NHS ester are typically characterized as part of the complete ADC. The PEG spacer provides enhanced solubility and reduces immunogenicity. The non-cleavable nature of the linker contributes to prolonged circulation time and reduced systemic toxicity of the ADC. The compound is typically stored at -20°C to maintain stability. Detailed PK parameters such as half-life, clearance, and volume of distribution depend on the specific antibody and payload used in the conjugate.
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| Toxicity/Toxicokinetics |
Mal-amido-PEG1-C2-NHS ester is a chemical reagent intended for research use only and is not approved for human therapeutic use. As a non-cleavable ADC linker, it is designed to maintain stable drug-antibody conjugation until internalization and degradation in target cells. The compound is typically stored at -20°C and handled with standard laboratory safety precautions. Toxicity studies are conducted on the complete ADC rather than the linker alone, and the safety profile depends on the specific antibody and payload combination.
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| References |
[1]. Hansen AM, et al. Microwave-assisted solid-phase synthesis of antisense acpP peptide nucleic acid-peptide conjugates active against colistin- and tigecycline-resistant E. coli and K. pneumoniae. Eur J Med Chem. 2019 Apr 15;168:134-145.
[2]. Zhang ge, et al. Preparation and application of FAPalpha activated polypeptide magnetic nanosphere compound used for diagnosis of tumors. CN105524141A |
| Additional Infomation |
Mal-amido-PEG1-C2-NHS ester is a non-cleavable ADC linker containing a maleimide group and an NHS ester, with molecular formula C16H19N3O8 and molecular weight 381.34. The NHS ester labels primary amines on proteins and other molecules, while the maleimide group conjugates to thiol groups. This linker is used in bioconjugation, drug delivery, and protein labeling applications. The PEG spacer provides solubility and flexibility. The compound is for research use only and has not been approved for clinical applications. Storage at -20°C is recommended for stability.
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| Molecular Formula |
C16H19N3O8
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|---|---|
| Molecular Weight |
381.3374
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| Exact Mass |
381.117
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| CAS # |
1260092-50-9
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| PubChem CID |
59257610
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| Appearance |
White to off-white solid powder
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| LogP |
-2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
27
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| Complexity |
653
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(=O)N(C1=O)OC(=O)CCOCCNC(=O)CCN2C(=O)C=CC2=O
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| InChi Key |
QXGYXAOYQWRQRZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19N3O8/c20-11(5-8-18-12(21)1-2-13(18)22)17-7-10-26-9-6-16(25)27-19-14(23)3-4-15(19)24/h1-2H,3-10H2,(H,17,20)
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]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 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) |
DMSO : 100 mg/mL (262.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.56 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 (6.56 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 (6.56 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 | 2.6223 mL | 13.1117 mL | 26.2233 mL | |
| 5 mM | 0.5245 mL | 2.6223 mL | 5.2447 mL | |
| 10 mM | 0.2622 mL | 1.3112 mL | 2.6223 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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