| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Disulfide Cleavable Linker
SPDMV targets the intracellular environment of cancer cells through its glutathione-cleavable mechanism. The disulfide bond in SPDMV is selectively cleaved by elevated glutathione levels found in tumor cells, enabling targeted drug release. As an ADC linker, SPDMV enables the conjugation of cytotoxic payloads to antibodies, facilitating selective delivery of drugs to cancer cells. The PEG spacer provides solubility and flexibility, reducing steric hindrance between the conjugated components. This design allows for efficient drug release specifically within the reducing environment of target cells. |
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| ln Vitro |
In vitro activity of SPDMV is assessed by its ability to form stable conjugates with antibodies and its selective cleavage in reducing environments. The efficiency of conjugation to antibodies is evaluated by SDS-PAGE, mass spectrometry, and HPLC. The cleavable nature of the disulfide bond is confirmed by incubation with glutathione or other reducing agents, followed by analysis of conjugate stability and drug release by HPLC or LC-MS. Cell binding and internalization studies are conducted using target-positive and target-negative cell lines to assess specificity and intracellular drug release.
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| ln Vivo |
In vivo studies for SPDMV are typically conducted as part of complete ADC development. The ADC is evaluated in mouse xenograft models bearing target-positive tumors. Efficacy is assessed by tumor growth inhibition, and pharmacokinetic studies evaluate the stability of the linker in circulation. The glutathione-cleavable nature of the disulfide bond is designed to maintain stability in the oxidative extracellular environment while enabling drug release in the reducing intracellular environment of tumor cells. This selective release mechanism enhances therapeutic index and reduces systemic toxicity.
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| Enzyme Assay |
For conjugation assays, SPDMV is dissolved in anhydrous DMSO or DMF and added to a solution of antibody or targeting protein in PBS buffer. The reaction is incubated at room temperature for 2-4 hours, and the extent of conjugation is monitored by SDS-PAGE or MALDI-TOF mass spectrometry. For glutathione cleavage studies, the conjugate is incubated with various concentrations of glutathione (0-10 mM) at 37°C, and the release of payload is analyzed by HPLC or LC-MS. The stability of the conjugate in plasma is assessed by incubation in mouse or human plasma at 37°C.
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| Cell Assay |
Target-positive cancer cell lines are cultured in appropriate media. Cells are treated with SPDMV-containing ADC conjugates at various concentrations for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays, and IC50 values are calculated. Cell binding is evaluated by flow cytometry using fluorescently labeled conjugates, and internalization is assessed using confocal microscopy or pH-sensitive dyes. For glutathione-dependent activity, cells are pretreated with glutathione synthesis inhibitors or modulators to confirm the cleavage mechanism.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice bearing target-positive tumor xenografts are administered the complete ADC (containing SPDMV as the linker) via intravenous injection. Dosing typically involves multiple injections at 1-2 week intervals. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity. At study termination, tumors and major organs are collected for histopathological analysis and drug concentration measurement. Pharmacokinetic studies assess ADC stability and drug release in circulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SPDMV are characterized as part of the complete ADC. The PEG spacer provides enhanced solubility and reduces immunogenicity. The glutathione-cleavable disulfide bond enables selective drug release in tumor cells while maintaining stability in circulation. The compound is typically stored at -20°C. Detailed PK parameters such as half-life, clearance, and volume of distribution depend on the specific antibody and payload used in the conjugate. The linker's performance in terms of stability and drug release kinetics is critical for ADC efficacy.
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| Toxicity/Toxicokinetics |
SPDMV is a chemical reagent intended for research use only and is not approved for human therapeutic use. As a glutathione-cleavable ADC linker, it is designed to enable selective drug release in tumor cells through cleavage of the disulfide bond triggered by elevated glutathione levels. The PEG-based linker provides solubility and flexibility. Toxicity studies are conducted on the complete ADC rather than the linker alone. Standard laboratory safety precautions should be followed when handling this compound. Storage at -20°C is recommended.
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| References | |
| Additional Infomation |
SPDMV is a glutathione-cleavable ADC linker with molecular formula C15H18N2O4S2 and molecular weight 354.44. It is a PEG-based linker used in the synthesis of antibody-drug conjugates. The disulfide bond enables selective cleavage in the reductive intracellular environment triggered by elevated glutathione levels in tumor cells. SPDMV is designed to remain stable in circulation while enabling targeted drug release. It is for research use only and has not been approved for clinical applications. Storage at -20°C is recommended.
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| Molecular Formula |
C15H18N2O4S2
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|---|---|
| Molecular Weight |
354.444421291351
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| Exact Mass |
354.07
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| CAS # |
890409-85-5
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| PubChem CID |
57901154
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| Appearance |
White to off-white solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
454
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCC(C)(C)SSC1C=CC=CN=1)ON1C(=O)CCC1=O
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| InChi Key |
GOJXFKVHNIGABU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H18N2O4S2/c1-15(2,23-22-11-5-3-4-10-16-11)9-8-14(20)21-17-12(18)6-7-13(17)19/h3-5,10H,6-9H2,1-2H3
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 4-methyl-4-(pyridin-2-yldisulfanyl)pentanoate
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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 (282.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.05 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 (7.05 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 (7.05 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 | 2.8214 mL | 14.1068 mL | 28.2135 mL | |
| 5 mM | 0.5643 mL | 2.8214 mL | 5.6427 mL | |
| 10 mM | 0.2821 mL | 1.4107 mL | 2.8214 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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