| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Mal-NH-ethyl-SS-propionic acid does not have a biological target itself; its function is chemical. It is a cleavable linker whose "target" is the reductive environment found inside cells. The disulfide bond in the linker is designed to be cleaved by intracellular reducing agents like glutathione (GSH). This property allows for the selective release of the cytotoxic payload inside the target cell, minimizing systemic toxicity. The maleimide group enables conjugation to thiol groups on the antibody, while the carboxylic acid provides a handle for attaching the drug payload.
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|---|---|
| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1].
In vitro, Mal-NH-ethyl-SS-propionic acid is not evaluated for biological activity. Its performance is characterized by its chemical reactivity and stability. Key parameters include its purity and its ability to form stable conjugates with antibodies and drug molecules. Its cleavability is often tested in vitro by incubating the complete ADC with reducing agents, such as glutathione or dithiothreitol (DTT), to simulate the intracellular environment. The release of the payload is then measured to confirm the linker's functionality. |
| ln Vivo |
In vivo, Mal-NH-ethyl-SS-propionic acid is not administered alone. Its function is realized as a component of an ADC. The linker's cleavability is designed to ensure that the cytotoxic payload is released specifically within the target cancer cell, after the ADC has been internalized. This targeted release is the cornerstone of ADC therapy, aiming to increase efficacy and reduce off-target toxicity. The linker's stability in circulation is also critical, as premature cleavage would lead to systemic release of the payload and increased toxicity.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies are not applicable to Mal-NH-ethyl-SS-propionic acid, as it is not a drug. Its characterization is primarily chemical. Standard analytical methods, including NMR and HPLC, are used to confirm its identity and purity. Its reactivity is assessed through conjugation efficiency assays, where its ability to couple with thiol- and amine-containing molecules is measured. Its cleavability is confirmed by exposing the linker or a conjugate to reducing conditions and analyzing the cleavage products.
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| Cell Assay |
In vitro cellular assays are not performed with Mal-NH-ethyl-SS-propionic acid alone. The activity of the linker is evaluated as part of a complete ADC. In these assays, cancer cells expressing the target antigen are treated with the ADC. The key readouts are cytotoxicity (cell viability assays like MTT or CellTiter-Glo) and the specificity of the effect, which is confirmed by comparing to a non-targeting control ADC. The success of the linker is demonstrated by potent and selective killing of target cells.
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| Animal Protocol |
In vivo animal studies for Mal-NH-ethyl-SS-propionic acid are not conducted on the linker alone. Its performance is evaluated through the in vivo efficacy of the complete ADC in xenograft mouse models. Tumor-bearing mice are treated with the ADC, and endpoints include tumor volume reduction, survival, and pharmacokinetic analysis. These studies are critical for demonstrating that the linker enables the ADC to deliver the payload effectively to the tumor while maintaining stability in circulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Mal-NH-ethyl-SS-propionic acid are not characterized independently. Its properties influence the PK of the complete ADC. Key characteristics include its molecular weight (332.4 g/mol), formula (C12H16N2O5S2), and the presence of the disulfide bond. The linker's stability in plasma is crucial for the ADC's circulation half-life, and its cleavage rate by intracellular reductants determines the rate of drug release. These properties are optimized to ensure the ADC has a favorable therapeutic index.
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| Toxicity/Toxicokinetics |
Toxicological data for Mal-NH-ethyl-SS-propionic acid are not available for the linker itself. Its safety profile is assessed as part of the complete ADC. The primary toxicity concerns are related to the cytotoxic payload and its potential for premature release. The use of a cleavable linker like this is intended to minimize systemic toxicity by ensuring the payload is released primarily within the target cells.
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| References | |
| Additional Infomation |
Mal-NH-ethyl-SS-propionic acid is a research-use-only chemical compound that serves as a crucial component in the development of ADCs. Its CAS number is 2128735-24-8. It is also known as a cleavable ADC linker. Its design as a cleavable linker with a disulfide bond is a common strategy in ADC technology, enabling targeted drug delivery and controlled release. It is not approved for human use and is strictly a research tool.
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| Molecular Formula |
C12H16N2O5S2
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|---|---|
| Molecular Weight |
332.395840644836
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| Exact Mass |
332.05
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| CAS # |
2128735-24-8
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| PubChem CID |
129627645
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| Appearance |
White to off-white solid powder
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| LogP |
0
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
21
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(CCNC(CCN1C(C=CC1=O)=O)=O)SCCC(=O)O
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| InChi Key |
MQYOVZAKKXDVHK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H16N2O5S2/c15-9(3-6-14-10(16)1-2-11(14)17)13-5-8-21-20-7-4-12(18)19/h1-2H,3-8H2,(H,13,15)(H,18,19)
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| Chemical Name |
3-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethyldisulfanyl]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: (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 (~300.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.52 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 (7.52 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 (7.52 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 | 3.0084 mL | 15.0421 mL | 30.0842 mL | |
| 5 mM | 0.6017 mL | 3.0084 mL | 6.0168 mL | |
| 10 mM | 0.3008 mL | 1.5042 mL | 3.0084 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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