| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Disulfide Cleavable Linker Cleavable Linker
The primary targets of S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate are the linker structures in ADC technology. As a glutathione-cleavable ADC linker, it connects the antibody to the cytotoxic payload through a disulfide bond that can be cleaved in the presence of intracellular glutathione. This allows for selective release of the payload inside target cells. The compound does not directly bind to enzymes or receptors but serves as a structural component. |
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| ln Vitro |
In vitro, S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate functions as a cleavable linker for ADC synthesis. The glutathione-cleavable nature allows for the selective release of the cytotoxic payload inside target cells where glutathione levels are elevated. The compound is used for attaching monoclonal antibodies (mAb) in ADCs. The linker itself does not exhibit direct cellular activity but enables the bioactivity of the conjugated therapeutic agent.
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| ln Vivo |
In vivo activity of S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is realized through the ADC constructs in which it is incorporated. As a glutathione-cleavable linker, it provides targeted release of the cytotoxic payload inside tumor cells. The linker's cleavability contributes to the overall efficacy and reduced off-target toxicity of the ADC. The in vivo efficacy depends on the specific antibody and payload used in the conjugate.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate focus on evaluating the stability and cleavage properties of the linker. The compound is incubated in buffer solutions with and without glutathione (0.1-10 mM) at 37°C. The cleavage of the linker is monitored by HPLC or LC-MS to detect the release of the payload. The glutathione-cleavable nature is confirmed by the presence of cleavage products in the presence of glutathione.
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| Cell Assay |
In vitro cellular assays for S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate involve testing the complete ADC molecule rather than the linker alone. Cancer cell lines are treated with the ADC, and cell viability is assessed using CCK-8 or MTT assays after 72 hours. The linker's contribution to ADC activity is evaluated by comparing the activity of the ADC with that of the unconjugated payload. The linker itself does not directly affect cell viability.
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| Animal Protocol |
In vivo animal studies for S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate are conducted using the final ADC construct. Tumor-bearing xenograft models receive the ADC via intravenous injection. Tumor volume and body weight are monitored over 2-4 weeks to assess efficacy and tolerability. The linker contributes to the stability and PK profile of the ADC. Detailed in vivo protocols are similar to those used for other ADC linkers.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate are determined by the ADC in which it is incorporated. The compound has a molecular weight of approximately 184.28 and a molecular formula of C₅H₁₂O₃S₂. It is a glutathione-cleavable linker, providing targeted release of the payload. The linker's cleavability contributes to the PK profile of the ADC, with payload release occurring primarily inside target cells.
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| Toxicity/Toxicokinetics |
The toxicity profile of S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is associated with the ADC in which it is used. As a linker compound, it is considered to have low intrinsic toxicity. Standard toxicity studies for the final ADC include assessment of body weight changes, clinical observations, hematological parameters, and histopathological examination of major organs in animal models. The linker itself does not exhibit significant cytotoxic effects.
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| References | |
| Additional Infomation |
S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate (CAS 2127875-65-2) has a molecular formula of C₅H₁₂O₃S₂ and a molecular weight of approximately 184.28. It is a glutathione-cleavable ADC linker used for antibody-drug conjugates. The compound appears as a colorless to light yellow ointment with a purity of ≥98%. It is intended for research use only and is not approved for clinical use. The linker is used for attaching monoclonal antibodies in ADCs.
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| Molecular Formula |
C5H12O3S2
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|---|---|
| Molecular Weight |
184.276979446411
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| Exact Mass |
184.022
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| CAS # |
2127875-65-2
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| PubChem CID |
145712389
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| Appearance |
Colorless to light yellow ointment
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| LogP |
0
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
10
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| Complexity |
187
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(CO)SS(=O)(=O)C
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| InChi Key |
DRRLIMMXMOWDCA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H12O3S2/c1-5(2,4-6)9-10(3,7)8/h6H,4H2,1-3H3
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| Chemical Name |
2-methyl-2-methylsulfonylsulfanylpropan-1-ol
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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 (542.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.57 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 (13.57 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 (13.57 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 | 5.4265 mL | 27.1326 mL | 54.2652 mL | |
| 5 mM | 1.0853 mL | 5.4265 mL | 10.8530 mL | |
| 10 mM | 0.5427 mL | 2.7133 mL | 5.4265 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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