| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
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| Targets |
Sulfo-LC-SPDP Crosslinker does not have a specific biological target in the traditional sense; it is a chemical tool for bioconjugation. It reacts with primary amines (e.g., lysine residues on proteins) via its sulfo-NHS-ester group, and with sulfhydryl groups (e.g., cysteine residues or reduced disulfides) via its 2-pyridyldithio group. This enables the formation of stable amide and disulfide bonds between molecules.
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| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1].
Sulfo-LC-SPDP is a chemical crosslinker, not a bioactive compound with direct pharmacological activity. Its "activity" is its ability to form covalent bonds between molecules containing amines and thiols. The sulfo-NHS-ester group reacts with primary amines to form stable amide bonds, while the pyridyldithio group reacts with sulfhydryl groups to form disulfide bonds. The disulfide bond is cleavable under reducing conditions (e.g., DTT or TCEP), allowing for controlled release. |
| ln Vivo |
Sulfo-LC-SPDP is not a drug and is not used in in vivo pharmacological studies as an active therapeutic agent. It is used as a tool for preparing bioconjugates, such as antibody-drug conjugates (ADCs), which are then evaluated in vivo. The crosslinker itself is not administered to animals for therapeutic purposes.
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| Enzyme Assay |
The reactivity of Sulfo-LC-SPDP Crosslinker can be characterized using in vitro biochemical assays. The efficiency of conjugation between amine-containing molecules (e.g., antibodies) and thiol-containing molecules (e.g., drugs) can be assessed by SDS-PAGE, size exclusion chromatography, or mass spectrometry. The amount of 2-pyridylthione released upon reaction with thiols can be measured spectrophotometrically at 343 nm to monitor the conjugation reaction.
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| Cell Assay |
In vitro cell-based assays are used to evaluate the activity of the bioconjugates prepared using Sulfo-LC-SPDP, not the crosslinker itself. For example, an antibody-drug conjugate (ADC) prepared with Sulfo-LC-SPDP is tested for cytotoxicity against target antigen-expressing cancer cell lines. Cells are treated with the ADC at various concentrations, and cell viability is assessed using MTT or CellTiter-Glo assays. The crosslinker enables the attachment of the drug to the antibody, allowing for targeted delivery.
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| Animal Protocol |
Sulfo-LC-SPDP is used as a linker to prepare antibody-drug conjugates (ADCs) for in vivo efficacy studies. The ADC is administered to tumor-bearing mice via intravenous injection, and tumor growth inhibition is monitored. The crosslinker itself is not administered directly; it is part of the ADC construct. The in vivo efficacy of the ADC depends on the targeting antibody, the payload drug, and the properties of the linker.
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| ADME/Pharmacokinetics |
Sulfo-LC-SPDP is a water-soluble crosslinker, which improves its compatibility with aqueous biological systems. It has a molecular weight of 505.59. The compound is typically stored as a solid at room temperature; powder can be stored at -20°C for 3 years or at 4°C for 2 years. In solvent, it can be stored at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Sulfo-LC-SPDP is a chemical reagent and should be handled with appropriate safety precautions. Specific toxicity data (e.g., LD50) are not typically determined for crosslinkers as they are not intended for therapeutic use. The compound may cause skin and eye irritation upon contact. Appropriate personal protective equipment (gloves, goggles, lab coat) should be worn when handling this chemical.
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| References | |
| Additional Infomation |
Sulfo-LC-SPDP Crosslinker (CAS# 169751-10-4) is also known by its sodium salt form, Sulfo-LC-SPDP sodium. The related CAS number for the non-sulfonated form is 150244-18-1. This NHS-activated crosslinker enables stable amide bond formation with primary amines and is widely used in bioconjugation, drug delivery, and targeted therapeutic development. It is a highly effective ADC linker designed for advanced ADC development and targeted cancer therapies.
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| Molecular Formula |
C18H23N3O8S3
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|---|---|
| Molecular Weight |
505.58552
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| Exact Mass |
527.047
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| CAS # |
169751-10-4
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| Related CAS # |
Sulfo-LC-SPDP;150244-18-1
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| PubChem CID |
4588467
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| Appearance |
White to off-white solid
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| Density |
1.53g/cm3
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| Melting Point |
185-187ºC
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| Index of Refraction |
1.64
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| LogP |
2.429
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
33
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| Complexity |
793
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCSSC1=CC=CC=N1)NCCCCCC(ON1C(=O)CC(S(=O)(O)=O)C1=O)=O
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| InChi Key |
ZAPNXDUFCQIHFS-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C18H23N3O8S3.Na/c22-14(8-11-30-31-15-6-3-5-10-20-15)19-9-4-1-2-7-17(24)29-21-16(23)12-13(18(21)25)32(26,27)28;/h3,5-6,10,13H,1-2,4,7-9,11-12H2,(H,19,22)(H,26,27,28);/q;+1/p-1
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| Chemical Name |
sodium;2,5-dioxo-1-[6-[3-(pyridin-2-yldisulfanyl)propanoylamino]hexanoyloxy]pyrrolidine-3-sulfonate
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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 (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 (~189.6 mM)
H2O: ~10 mg/mL (~19.0 mM; with ultrasonication) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 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 (4.74 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 (4.74 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 | 1.9779 mL | 9.8894 mL | 19.7789 mL | |
| 5 mM | 0.3956 mL | 1.9779 mL | 3.9558 mL | |
| 10 mM | 0.1978 mL | 0.9889 mL | 1.9779 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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