| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Disulfide Cleavable Linker Cleavable Linker
SPDV has no direct biological target. As an ADC linker, it facilitates the conjugation of antibodies (or other targeting ligands) to cytotoxic payloads. The pyridyl disulfide group reacts with thiols (e.g., from engineered cysteine residues or reduced interchain disulfides) on antibodies, forming a disulfide bond that can be cleaved in the reducing environment of the intracellular compartment, releasing the payload inside target cells. |
|---|---|
| ln Vitro |
Not applicable; SPDV is a synthetic building block with no inherent biological activity. Its utility is indirectly demonstrated through the in vitro activity of complete ADCs formed using this linker. Antigen‑positive cancer cells incubated with ADCs containing SPDV typically show potent and selective cytotoxicity, confirming successful payload conjugation and intracellular release.
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| ln Vivo |
Not applicable; SPDV alone is not administered in vivo. ADCs constructed with SPDV are evaluated in mouse xenograft tumor models. SPDV‑based ADCs have been shown to have improved efficacy and reduced toxicity compared to ADCs built with other linkers, likely due to controlled intracellular drug release. For example, anti‑CD22‑SPDV‑maytansine ADCs (e.g., pinatuzumab vedotin‑like constructs) show antitumor activity in lymphoma models.
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| Enzyme Assay |
Not applicable; SPDV is not used in enzyme/receptor binding assays. However, the cleavability of the pyridyl disulfide bond can be demonstrated in vitro by incubating SPDV (or a model conjugate) with reducing agents such as 10 mM dithiothreitol (DTT) or 5 mM glutathione (GSH) at 37 degC for 30-60 min. The release of pyridine‑2‑thione is monitored spectrophotometrically at 343 nm.
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| Cell Assay |
Not applicable; SPDV is not tested directly on cells. For the functional evaluation of an ADC prepared with SPDV, antigen‑positive cancer cells (e.g., CD22‑positive Ramos cells or HER2‑positive SK‑BR‑3 cells) are treated with the ADC (0.001-100 nM) for 72-96 h. Cell viability is measured by CellTiter‑Glo or MTT. Selective killing of antigen‑positive over antigen‑negative cells confirms proper conjugation and release.
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| Animal Protocol |
Not applicable; SPDV alone is not evaluated in animals. ADCs employing SPDV are typically administered intravenously at 1-10 mg/kg once weekly for 2-4 weeks in mouse xenograft models. Tumor volume is measured twice weekly. Safety is monitored through body weight changes and serum chemistry. The efficacy and tolerability of SPDV‑based ADCs are generally favorable, with the cleavable disulfide linker allowing for efficient payload release in the intracellular reducing environment.
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| ADME/Pharmacokinetics |
Not applicable; SPDV is a chemical linker not intended for standalone administration. For ADCs incorporating SPDV, the linker contributes to a pharmacokinetic profile characterized by stability in circulation (due to limited reducing capacity in plasma) and efficient cleavage inside cells (due to high intracellular GSH concentration). Complete ADC clearance and half‑life are determined by the antibody component, typically several days.
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| Toxicity/Toxicokinetics |
Not applicable; SPDV is not a drug substance and is not tested in standalone toxicology studies. ADCs constructed with SPDV may have a safety profile influenced by payload characteristics and targeting specificity. The cleavable disulfide bond may reduce systemic toxicity compared to non‑cleavable linkers by limiting premature release of cytotoxic payload in circulation.
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| References | |
| Additional Infomation |
SPDV is a research‑grade chemical reagent used in ADC development, particularly for preparing conjugates with disulfide‑linkable payloads such as maytansinoids and auristatins. It is not a therapeutic agent and has not been approved for human use. The compound is related to the SPDB (N‑succinimidyl 4‑(2‑pyridyldithio)butyrate) family of linkers but contains a longer pentanoate spacer, which may improve conjugation efficiency. No clinical trials are registered for SPDV itself.
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| Molecular Formula |
C14H16N2O4S2
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|---|---|
| Molecular Weight |
340.42
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| Exact Mass |
340.055
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| CAS # |
317331-86-5
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| PubChem CID |
87534914
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| Appearance |
White to off-white solid powder
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
22
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| Complexity |
404
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(ON1C(CCC1=O)=O)CCCCSSC2=NC=CC=C2
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| InChi Key |
ABQGFYSYSCHJNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N2O4S2/c17-12-7-8-13(18)16(12)20-14(19)6-2-4-10-21-22-11-5-1-3-9-15-11/h1,3,5,9H,2,4,6-8,10H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 5-(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 (293.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 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 (7.34 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 (7.34 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 | 2.9375 mL | 14.6877 mL | 29.3755 mL | |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 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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