| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Non-cleavable Linker for Antibody-drug conjugates (ADC)
BS3 Crosslinker disodium is classified as a non-cleavable ADC linker. The compound targets primary amine groups (-NH₂) on proteins, including the lysine residues of antibodies. The sulfo-NHS ester groups react with primary amines to form stable amide bonds. The crosslinker contains two reactive groups connected by a spacer arm, allowing it to crosslink two proteins or to attach a payload to an antibody. The non-cleavable nature of the linker means that the conjugate remains intact until the antibody is degraded. |
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| ln Vitro |
ADC is made up of antibodies that have an ADC linker connecting them to the ADC cytotoxin [1].
In vitro, BS3 Crosslinker disodium is used for the synthesis of ADCs. ADCs consist of an antibody attached to an ADC cytotoxin through an ADC linker. The compound’s water solubility and amine reactivity make it suitable for conjugation reactions in aqueous buffers. The sulfo-NHS ester groups react efficiently with primary amines at pH 7-9 to form stable amide bonds. The compound’s non-cleavable nature ensures that the ADC remains stable in circulation. |
| ln Vivo |
No detailed in vivo activity data for BS3 Crosslinker disodium has been published in the available literature. The compound is a research tool used primarily for the synthesis of ADCs. Its in vivo activity would depend on the specific antibody and cytotoxin to which it is conjugated. The non-cleavable nature of the linker means that the conjugate remains intact until the antibody is degraded.
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| Enzyme Assay |
The conjugation efficiency of BS3 Crosslinker disodium can be assessed using various analytical techniques. In a typical conjugation reaction, the antibody is buffer-exchanged into a suitable conjugation buffer (pH 7-9). BS3 Crosslinker disodium is dissolved in water or DMSO and added to the antibody at a defined molar ratio. The reaction is incubated at room temperature for 30-60 minutes. The degree of conjugation is assessed by MALDI-TOF mass spectrometry or by SDS-PAGE. The purity of the conjugate is assessed by size exclusion chromatography (SEC).
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| Cell Assay |
The cellular activity of BS3 Crosslinker disodium conjugates is assessed in cell-based assays that depend on the specific antibody and cytotoxin. For ADC applications, the antibody-drug conjugate is added to target cells expressing the appropriate antigen. Cell viability is measured using MTT or CellTiter-Glo assays. The specificity of the conjugate for target cells is assessed by comparing activity against antigen-positive and antigen-negative cell lines.
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| Animal Protocol |
No detailed in vivo animal model data for BS3 Crosslinker disodium has been published in the available literature. The compound is a research tool used in the synthesis of ADCs. Its in vivo efficacy would be evaluated in animal models using the specific ADC to which it is conjugated. Typical studies would involve xenograft models for ADC efficacy.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data for BS3 Crosslinker disodium has been published in the available literature. The compound has a molecular weight of 572.43 g/mol, a molecular formula of C16H18N2Na2O14S2. It is soluble in DMSO at 125 mg/mL (218.37 mM). The compound is typically stored as a powder at -20°C, protected from moisture and light. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. Further studies would be needed to characterize the pharmacokinetic properties of BS3 Crosslinker disodium conjugates.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for BS3 Crosslinker disodium has been published in the available literature. As a research compound used in ADC synthesis, BS3 Crosslinker disodium is not intended for direct therapeutic use. The toxicity of BS3 Crosslinker disodium conjugates would depend on the specific antibody and cytotoxin. The compound is typically handled with standard laboratory safety precautions.
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| References | |
| Additional Infomation |
Antibody-drug conjugates (ADCs) are among the fastest-growing drugs in the field of cancer treatment. After half a century of research, the approval of brentuximab (2011) and trastuzumab (2013) paved the way for ongoing clinical trials that are evaluating more than 60 other ADC candidates. Limited success of first-generation ADCs (developed in the early 21st century) has prompted the development of strategies to bring second-generation ADCs to market. Second-generation ADCs have higher levels of cytotoxic drug conjugation, lower levels of naked antibody, and more stable drug-antibody linkers. In addition, experience accumulated over the past decade is being used to develop third-generation ADCs. In this review, we will discuss how to select the best target antigen and appropriate cytotoxic drug; optimize the design of linkers; discover bioorthogonal coupling chemistry; and toxicity issues. The focus of antibody-drug conjugate (ADC) research is on selecting and modifying antibodies for site-specific drug conjugation, which will lead to higher uniformity and stability, as well as exploring new coupling chemistry and mechanisms of action. [1]
BS3 Crosslinker disodium (CAS#: 127634-19-9) is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The compound is a homobifunctional sulfo-NHS ester that reacts with primary amines on proteins to form stable amide bonds. It has a molecular weight of 572.43 g/mol and a molecular formula of C16H18N2Na2O14S2. The compound is water-soluble, making it suitable for conjugation reactions in aqueous solutions. It is typically stored at -20°C, protected from moisture and light. BS3 Crosslinker disodium is a valuable tool for protein crosslinking and bioconjugation applications. |
| Molecular Formula |
C16H18N2NA2O14S2
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|---|---|
| Molecular Weight |
572.43
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| Exact Mass |
571.999
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| CAS # |
127634-19-9
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| Related CAS # |
BS3 Crosslinker;82436-77-9
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| PubChem CID |
6097991
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
36
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| Complexity |
987
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(C(=O)N(C1=O)OC(=O)CCCCCCC(=O)ON2C(=O)CC(C2=O)S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+]
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| InChi Key |
MGJYOHMBGJPESL-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C16H20N2O14S2.2Na/c19-11-7-9(33(25,26)27)15(23)17(11)31-13(21)5-3-1-2-4-6-14(22)32-18-12(20)8-10(16(18)24)34(28,29)30;;/h9-10H,1-8H2,(H,25,26,27)(H,28,29,30);;/q;2*+1/p-2
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| Chemical Name |
disodium;1-[8-(2,5-dioxo-3-sulfonatopyrrolidin-1-yl)oxy-8-oxooctanoyl]oxy-2,5-dioxopyrrolidine-3-sulfonate
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| Synonyms |
127634-19-9; Bis(sulfosuccinimidyl) suberate sodium salt; BS3 Crosslinker; Suberate Bis(sulfosuccinimidyl) Sodium Salt; Suberate Bis(sulfosuccinimidyl) Sodium Salt (~85%); Sodium 1,1'-(octanedioylbis(oxy))bis(2,5-dioxopyrrolidine-3-sulfonate); BS3; BS3 Crosslinker (disodium);
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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 and light. |
| 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 : 125 mg/mL (218.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.63 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 20.8 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: ≥ 2.08 mg/mL (3.63 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 20.8 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: ≥ 2.08 mg/mL (3.63 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 | 1.7469 mL | 8.7347 mL | 17.4694 mL | |
| 5 mM | 0.3494 mL | 1.7469 mL | 3.4939 mL | |
| 10 mM | 0.1747 mL | 0.8735 mL | 1.7469 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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