| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Azidoethyl-SS-ethylazide itself does not bind to a specific biological target. As a cleavable ADC linker, it connects an antibody to a cytotoxic payload. The disulfide bond enables redox-sensitive drug release in the intracellular environment. The azide groups enable click chemistry conjugation.
|
|---|---|
| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1].
In vitro activity is primarily related to its function as an ADC linker. It enables the formation of stable conjugates via click chemistry. ADCs synthesized using this linker deliver cytotoxic payloads to target cells. The cleavable nature allows for payload release in the intracellular environment. No direct pharmacological activity is attributed to the linker itself. |
| ln Vivo |
In vivo activity is inferred from the performance of ADCs synthesized using this linker. ADCs incorporating this linker deliver payloads to target cells and release them in the intracellular environment. The cleavable disulfide bond enables redox-sensitive drug release. No direct in vivo activity is associated with the linker alone.
|
| Enzyme Assay |
In vitro assays for Azidoethyl-SS-ethylazide typically involve evaluating the efficiency of click chemistry conjugation. The azide groups are reacted with alkyne-containing molecules in the presence of copper catalysts or with DBCO/BCN groups in copper-free reactions. Reaction progress is monitored by HPLC, mass spectrometry, or NMR. Purity is assessed by HPLC. The disulfide bond can be cleaved by reducing agents.
|
| Cell Assay |
Cell-based assays for Azidoethyl-SS-ethylazide are conducted in the context of the final ADC molecule. Cells expressing the target antigen are treated with the ADC, and cytotoxicity is measured by MTT or CellTiter-Glo assays. Antigen-specific cell killing is compared to non-targeting controls. Internalization and trafficking of the ADC are assessed by immunofluorescence microscopy.
|
| Animal Protocol |
In vivo animal studies are performed with ADCs containing this linker. Tumor-bearing mice are treated with the ADC, and tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring ADC levels in blood and tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters. The cleavable nature of the linker is evaluated for payload release at the tumor site.
|
| ADME/Pharmacokinetics |
Azidoethyl-SS-ethylazide (molecular weight 204.28, formula C4H8N6S2) is a cleavable ADC linker. It is soluble in DMSO at 10 mM. It is stored at -20°C. No specific PK data are available for this linker alone; its PK profile is determined by the conjugated molecule.
|
| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Azidoethyl-SS-ethylazide. The compound is for research use only and not intended for therapeutic use. Standard laboratory safety precautions should be followed. The disulfide bond may present additional considerations for handling. Store at -20°C.
|
| References |
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
|
| Additional Infomation |
Azidoethyl-SS-ethylazide (CAS#: 352305-38-5) is a bifunctional cleavable ADC linker with azide and disulfide groups. It enables bioorthogonal conjugation and redox-sensitive drug release. Molecular weight: 204.28, formula: C4H8N6S2.
|
| Molecular Formula |
C4H8N6S2
|
|---|---|
| Molecular Weight |
204.277
|
| Exact Mass |
204.025
|
| CAS # |
352305-38-5
|
| PubChem CID |
85789208
|
| Appearance |
Colorless to light yellow liquid
|
| LogP |
2.7
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
12
|
| Complexity |
172
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(CSSCCN=[N+]=[N-])N=[N+]=[N-]
|
| InChi Key |
SYKSDZXTWAVSIP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C4H8N6S2/c5-9-7-1-3-11-12-4-2-8-10-6/h1-4H2
|
| Chemical Name |
1-azido-2-(2-azidoethyldisulfanyl)ethane
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8952 mL | 24.4762 mL | 48.9524 mL | |
| 5 mM | 0.9790 mL | 4.8952 mL | 9.7905 mL | |
| 10 mM | 0.4895 mL | 2.4476 mL | 4.8952 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
