| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Targets |
As an ADC linker, Aminoethyl-SS-propionic acid does not have a traditional biological target. Its role is to connect a cytotoxic drug (payload) to a monoclonal antibody. The disulfide bond is the key functional group that is cleaved in the intracellular environment, releasing the active drug. This makes it a "cleavable linker". The linker's stability in circulation and efficient cleavage inside the target cell are critical for its function.
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| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1].
In vitro, Aminoethyl-SS-propionic acid is used as a linker to create functional ADCs. The resulting conjugates exhibit specific cytotoxicity against target antigen-expressing cancer cells. For example, ADCs made with this linker and a membrane-impermeable cytotoxin have been shown to inhibit HER2 dimerization and induce cytotoxicity in HER2-positive breast cancer cells. The linker's ability to release the drug intracellularly is confirmed in these cell-based assays. |
| ln Vivo |
In vivo, the efficacy of ADCs constructed with Aminoethyl-SS-propionic acid would be evaluated in animal models. The disulfide linker is designed to be stable in the bloodstream but cleaved once the ADC is internalized into the target cell, allowing for selective delivery of the cytotoxic payload. This targeted approach aims to improve the therapeutic index of potent anticancer drugs by reducing systemic toxicity. The linker's performance is a key factor in the ADC's overall efficacy and safety.
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| Enzyme Assay |
In vitro assays for Aminoethyl-SS-propionic acid typically involve testing the complete ADC, not the linker alone. The stability of the disulfide bond can be assessed in vitro by incubating the ADC in reducing conditions (e.g., with glutathione or DTT) and analyzing the released drug by HPLC or mass spectrometry. Its stability in plasma can also be assessed. These methods are for reference only.
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| Cell Assay |
In vitro cell-based assays for ADCs containing Aminoethyl-SS-propionic acid evaluate their cytotoxicity and specificity. Target antigen-positive and antigen-negative cell lines are treated with the ADC. Cell viability is assessed using MTT or CellTiter-Glo assays to determine the IC₅₀. The specificity of the ADC for the target antigen is confirmed by comparing its activity on positive vs. negative cells. The mechanism of cell death (e.g., apoptosis) can also be investigated. Standard cell culture conditions are used.
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| Animal Protocol |
In vivo animal studies for ADCs containing Aminoethyl-SS-propionic acid utilize xenograft mouse models bearing human tumors that express the target antigen. The ADC is administered intravenously at various doses. Tumor growth inhibition is monitored, and survival is recorded. Pharmacokinetic studies assess the stability and half-life of the ADC in circulation. Pharmacodynamic studies evaluate target engagement and the release of the payload in the tumor. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Aminoethyl-SS-propionic acid are not characterized independently, as it is part of an ADC. The properties of the linker influence the overall ADC's PK, such as its stability in circulation and rate of clearance. The disulfide bond can be cleaved by thiols in the blood, leading to payload release. The linker's hydrophilicity also affects the ADC's aggregation and solubility.
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| Toxicity/Toxicokinetics |
The toxicity profile of Aminoethyl-SS-propionic acid is evaluated as part of the ADC. The linker is designed to be stable and non-toxic in circulation. Its cleavage products are the antibody and the payload, whose toxicity is well-characterized. Off-target toxicity is minimized by the targeted delivery mechanism. However, premature cleavage of the disulfide bond can lead to systemic toxicity.
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| References | |
| Additional Infomation |
Additional information: Aminoethyl-SS-propionic acid has the CAS number 15579-00-7. Its molecular formula is C₅H₁₁NO₂S₂ and its molecular weight is 181.28 g/mol. It is a cleavable ADC linker. Its disulfide bond is sensitive to thiols, enabling selective intracellular drug release. It is a research tool for developing targeted cancer therapies. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C5H11NO2S2
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|---|---|
| Molecular Weight |
181.27634
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| Exact Mass |
181.023
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| CAS # |
15579-00-7
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| PubChem CID |
5195062
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| Appearance |
White to off-white solid powder
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| Density |
1.32g/cm3
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| Boiling Point |
339.5ºC at 760 mmHg
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| Melting Point |
138-141ºC
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| Flash Point |
159.1ºC
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| Vapour Pressure |
1.69E-05mmHg at 25°C
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| Index of Refraction |
1.589
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| LogP |
1.501
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
10
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| Complexity |
99.6
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HMMFDEBVQNRZLJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H11NO2S2/c6-2-4-10-9-3-1-5(7)8/h1-4,6H2,(H,7,8)
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| Chemical Name |
3-(2-aminoethyldisulfanyl)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 |
| 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) |
H2O : ~125 mg/mL (~689.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 11.11 mg/mL (61.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5163 mL | 27.5816 mL | 55.1633 mL | |
| 5 mM | 1.1033 mL | 5.5163 mL | 11.0327 mL | |
| 10 mM | 0.5516 mL | 2.7582 mL | 5.5163 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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