| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Mal-PEG2-NHS ester does not have a biological target; it is a chemical linker. Its "target" is the functional groups on biomolecules. The maleimide group provides a site for selective conjugation to thiol groups, while the NHS ester reacts with primary amines. This allows it to act as a bridge in ADCs, linking the antibody to the cytotoxic payload. Its non-cleavable nature is a key design feature for stable drug delivery.
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|---|---|
| ln Vitro |
In vitro, Mal-PEG2-NHS ester is not evaluated for biological activity. Its performance is characterized by its chemical reactivity. Key parameters include its purity (≥95%) and its ability to form stable conjugates. The PEG spacer increases solubility. Its reactivity is confirmed through conjugation efficiency assays.
|
| ln Vivo |
In vivo, Mal-PEG2-NHS ester is not administered alone. As a non-cleavable linker, it is used in ADCs where the payload is released after the antibody is degraded inside the target cell. Its stability in circulation is critical to prevent premature release.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies are not applicable to Mal-PEG2-NHS ester. Its characterization is chemical. Standard analytical methods, including NMR and HPLC, are used to confirm its identity and purity.
|
| Cell Assay |
In vitro cellular assays are not performed with Mal-PEG2-NHS ester alone. When incorporated into an ADC, its performance is evaluated in cell-based assays. The key readout is the specific killing of target cells.
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| Animal Protocol |
In vivo animal studies for Mal-PEG2-NHS ester are not conducted on the linker alone. Its performance is evaluated through the in vivo efficacy of the complete ADC in animal models, such as xenograft mouse models. Endpoints include tumor growth inhibition and survival.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Mal-PEG2-NHS ester are not characterized independently. Its properties influence the PK of the complete conjugate. Key characteristics include its molecular weight (354.31 g/mol) and formula (C15H18N2O8).
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| Toxicity/Toxicokinetics |
Mal-PEG2-NHS ester is a research chemical and is not intended for human therapeutic use. As a chemical reagent, it should be handled with appropriate laboratory safety precautions. Toxicity studies are not typically conducted for such linkers.
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| References |
Sano K, Nakajima T, Miyazaki K, Ohuchi Y, Ikegami T, Choyke PL, Kobayashi H. Short PEG-linkers improve the performance of targeted, activatable monoclonal antibody-indocyanine green optical imaging probes. Bioconjug Chem. 2013 May 15;24(5):811-6. doi: 10.1021/bc400050k. Epub 2013 May 3. PubMed PMID: 23600922; PubMed Central PMCID: PMC3674550.
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| Additional Infomation |
Mal-PEG2-NHS ester is a research-use-only chemical building block used as a non-cleavable ADC linker. Its CAS number is 1433997-01-3. It is a fundamental tool in the field of targeted therapy development and is not approved for clinical use.
|
| Molecular Formula |
C15H18N2O8
|
|---|---|
| Molecular Weight |
354.312024593353
|
| Exact Mass |
354.106
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| CAS # |
1433997-01-3
|
| Related CAS # |
1433997-01-3
|
| PubChem CID |
59129882
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| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
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| Boiling Point |
524.3±60.0 °C at 760 mmHg
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| Flash Point |
270.9±32.9 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.566
|
| LogP |
-1.9
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
25
|
| Complexity |
566
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(ON1C(CCC1=O)=O)CCOCCOCCN2C(C=CC2=O)=O
|
| InChi Key |
KMEJZQCDHANYJV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H18N2O8/c18-11-1-2-12(19)16(11)6-8-24-10-9-23-7-5-15(22)25-17-13(20)3-4-14(17)21/h1-2H,3-10H2
|
| Chemical Name |
2,5-dioxopyrrolidin-1-yl 3-(2-(2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethoxy)ethoxy)propanoate
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| Synonyms |
Mal-PEG2 NHS esterMal-PEG2-NHS ester
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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 (~282.24 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.06 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 (7.06 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 (7.06 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 | 2.8224 mL | 14.1119 mL | 28.2239 mL | |
| 5 mM | 0.5645 mL | 2.8224 mL | 5.6448 mL | |
| 10 mM | 0.2822 mL | 1.4112 mL | 2.8224 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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