| Size | Price | |
|---|---|---|
| 500mg | ||
| Other Sizes |
Purity: ≥97%
| Targets |
AMAS targets amine and sulfhydryl groups for covalent conjugation. As a heterobifunctional crosslinker, it contains an NHS ester that reacts with primary amines and a maleimide group that reacts with sulfhydryl groups. This allows for the formation of stable amide and thioether bonds between molecules. AMAS is a non-cleavable crosslinker, meaning the bonds formed are not reversible. It is widely used in ADC development for linking antibodies to cytotoxic payloads.
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|---|---|
| ln Vitro |
In vitro, AMAS is used for covalent conjugation of amine- and sulfhydryl-containing molecules. It is a non-cleavable heterobifunctional crosslinker with NHS ester and maleimide groups. The compound is widely used in antibody-drug conjugate (ADC) development. Its crosslinking efficiency has been characterized in various in vitro conjugation assays. AMAS is used to link antibodies to cytotoxic drugs for targeted therapy.
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| ln Vivo |
In vivo, AMAS is used in the development of antibody-drug conjugates (ADCs) for targeted cancer therapy. As a non-cleavable crosslinker, it enables stable conjugation of antibodies to cytotoxic payloads. The compound is used in preclinical research for ADC development. Further in vivo studies have evaluated the efficacy and safety of AMAS-based ADCs in animal models.
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| Enzyme Assay |
AMAS crosslinking assays involve measuring conjugation efficiency between amine- and sulfhydryl-containing molecules. The compound is incubated with amine-containing molecules (e.g., antibodies) and sulfhydryl-containing molecules (e.g., cytotoxic drugs) under appropriate conditions. Conjugation efficiency is assessed by SDS-PAGE, HPLC, or mass spectrometry. The formation of amide and thioether bonds is confirmed. Assays are performed in appropriate buffer systems with positive controls such as known crosslinkers.
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| Cell Assay |
AMAS cell-based assays are conducted in cancer cell lines for ADC efficacy studies. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with AMAS-based ADCs at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Target antigen expression is confirmed by flow cytometry. ADC internalization and cytotoxicity are assessed. Experiments are performed in triplicate with appropriate positive (e.g., known ADCs) and negative (vehicle) controls.
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| Animal Protocol |
AMAS in vivo studies are conducted in mouse models of cancer for ADC efficacy evaluation. Tumor-bearing mice are treated with AMAS-based ADCs via intravenous injection. Tumor growth is monitored by caliper measurements. Survival rates are monitored. Pharmacokinetic parameters are determined from plasma samples. For toxicology studies, animals are monitored for adverse effects. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
AMAS (MW 252.18 g/mol, C10H8N2O6) is a heterobifunctional crosslinker. It is also known as Maleimidoacetic acid N-hydroxysuccinimide ester. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. AMAS is a non-cleavable crosslinker with NHS ester and maleimide groups. Pharmacokinetic parameters would be determined in species-specific studies. The compound is widely used in ADC development.
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| Toxicity/Toxicokinetics |
AMAS is generally well-tolerated in preclinical studies at doses used for ADC development. The compound is a heterobifunctional crosslinker with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| Additional Infomation |
AMAS is a non-cleavable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules. It is widely used in antibody-drug conjugate (ADC) development. AMAS enables stable conjugation of antibodies to cytotoxic payloads. Its molecular formula is C10H8N2O6 with a molecular weight of 252.18 g/mol. All applications are limited to non-human research use.
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| Molecular Formula |
C10H8N2O6
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|---|---|
| Molecular Weight |
252.1803
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| Exact Mass |
252.038
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| CAS # |
55750-61-3
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| PubChem CID |
3299229
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
430.1±47.0 °C at 760 mmHg
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| Melting Point |
174-175ºC
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| Flash Point |
213.9±29.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.620
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| LogP |
-2.21
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
461
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TYKASZBHFXBROF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8N2O6/c13-6-1-2-7(14)11(6)5-10(17)18-12-8(15)3-4-9(12)16/h1-2H,3-5H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 2-(2,5-dioxopyrrol-1-yl)acetate
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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 (~396.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.91 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 (9.91 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 (9.91 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 | 3.9654 mL | 19.8271 mL | 39.6542 mL | |
| 5 mM | 0.7931 mL | 3.9654 mL | 7.9308 mL | |
| 10 mM | 0.3965 mL | 1.9827 mL | 3.9654 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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