| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
As an ADC linker, (2S)-N3-IsoSer does not have a traditional biological target (e.g., enzyme, receptor) itself but serves as a chemical scaffold. It is a bifunctional molecule that covalently conjugates a cytotoxic payload (drug) to an antibody via stable triazole linkages. Its target is determined by the antibody it is conjugated to.
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| ln Vitro |
As an ADC linker component, the "activity" is measured by the efficiency of conjugation reactions. The azide group on (2S)-N3-IsoSer reacts specifically with alkyne-bearing molecules (e.g., DBCO, BCN) in a bioorthogonal manner, allowing site-specific drug attachment without interfering with the antibody's antigen-binding affinity.
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| ln Vivo |
In vivo activity is dependent on the complete ADC. The (2S)-N3-IsoSer linker provides stability in circulation to prevent premature payload release. Once the ADC binds to its target antigen on cancer cells and is internalized, the linker is cleaved by lysosomal enzymes, releasing the active cytotoxic payload. Efficacy is measured by tumor regression in xenograft models.
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| Enzyme Assay |
For copper-catalyzed azide-alkyne cycloaddition (CuAAc), (2S)-N3-IsoSer is mixed with an alkyne-terminated molecule in the presence of copper(I) catalyst (e.g., CuSO4/sodium ascorbate) and a ligand (e.g., THPTA) in a suitable buffer (pH 7-8). The reaction is incubated at room temperature for 1-2 hours, and progress is monitored by LC-MS or TLC to ensure >95% conversion.
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| Cell Assay |
Standard conjugation assays are performed using purified monoclonal antibodies (mAbs). The mAb is first functionalized with an alkyne group. Then, (2S)-N3-IsoSer DCHA is reacted with the alkyne-functionalized mAb under copper-free click conditions using a strained alkyne. The reaction is carried out at 37degC for 12-24 hours. Conjugation efficiency is assessed by LC-MS or HIC-HPLC.
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| Animal Protocol |
In vivo efficacy studies for ADCs built with this linker are typically performed in subcutaneous xenograft mouse models. Tumor-bearing mice are treated intravenously with the ADC (e.g., 3-10 mg/kg) every 4-7 days for 2-4 cycles. Tumor volume and body weight are measured twice weekly. Terminal blood samples are collected for pharmacokinetic assessment of ADC stability.
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| ADME/Pharmacokinetics |
As a small-molecule building block, (2S)-N3-IsoSer DCHA itself has high solubility in organic solvents. Upon incorporation into an ADC, the resulting conjugate exhibits favorable PK properties, including reduced systemic clearance, prolonged half-life (days), and enhanced tumor accumulation via the enhanced permeability and retention (EPR) effect or active targeting.
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| Toxicity/Toxicokinetics |
(2S)-N3-IsoSer is designed for chemical synthesis and conjugation applications; as such, its intrinsic toxicity is low. It is not used as a therapeutic agent alone but as a linker. In ADC context, toxicity primarily derives from the cytotoxic payload. Linker-related toxicity is minimal, as it is a non-toxic, biodegradable scaffold designed for site-specific drug delivery.
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| References | |
| Additional Infomation |
(2S)-N3-IsoSer DCHA is a specialized research chemical used exclusively for non-human research in drug discovery. It is not a clinical drug candidate by itself and has not been approved by the FDA or any other regulatory agency for human therapeutic use. It is a key enabler technology for the construction of next-generation ADCs and targeted therapies.
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| Molecular Formula |
C15H28N4O3
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|---|---|
| Molecular Weight |
312.41
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| Related CAS # |
(2S)-N3-IsoSer;1620171-65-4
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| Appearance |
Solid powder
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| SMILES |
OC([C@@H](O)CN=[N+]=[N-])=O.C1(CCCCC1)NC2CCCCC2
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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: Please store this product in a sealed and protected environment, 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 (~320.1 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (8.00 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2009 mL | 16.0046 mL | 32.0092 mL | |
| 5 mM | 0.6402 mL | 3.2009 mL | 6.4018 mL | |
| 10 mM | 0.3201 mL | 1.6005 mL | 3.2009 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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