| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Thiol groups on proteins, peptides, or biomolecules. The dibromomaleimide group is a reactive electrophile that undergoes a substitution reaction with thiol groups (-SH) to form stable thioether bonds. This reactivity allows DBM-C5-COOH to be used as a linker to conjugate two molecules, such as an antibody and a cytotoxic payload (e.g., MMAF) in ADC synthesis. The C5 spacer provides distance and flexibility between the two conjugated moieties. It is a chemical tool for bioconjugation.
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| ln Vitro |
Dibromomaleimide-C5-COOH itself is not evaluated for direct biological activity as it is a linker used in bioconjugation. Its activity is demonstrated when it is used to conjugate a targeting moiety (like an antibody) to a cytotoxic drug (like MMAF) to form an ADC. The resulting ADC is then tested for its ability to bind to target antigens on cancer cells and exert cytotoxicity. The linker's stability and efficiency in conjugation are assessed in vitro. It is a chemical building block.
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| ln Vivo |
In vivo activity is not applicable to Dibromomaleimide-C5-COOH itself as it is a linker for ADC synthesis. The in vivo efficacy would be attributed to the complete ADC molecule synthesized using this linker. Such ADCs would be evaluated in animal models for antitumor activity and pharmacokinetics. The compound itself is not administered to animals. Its role is confined to chemical synthesis. It is stored and handled based on its chemical properties.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to Dibromomaleimide-C5-COOH as it is a linker, not a drug candidate. The primary in vitro characterization involves the conjugation reaction. The linker is reacted with a thiol-containing molecule (e.g., a reduced antibody or a drug with a thiol group) in a buffer solution. The progress of the reaction is monitored by HPLC or mass spectrometry. The efficiency of conjugation and the stability of the resulting conjugate are assessed. No receptor binding assays are performed on the linker itself.
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| Cell Assay |
Cell-based assays are not directly performed on Dibromomaleimide-C5-COOH as it is a linker. However, the final ADC molecules synthesized using this linker are tested in cell-based assays. Typically, cancer cell lines expressing the target antigen are treated with the ADC, and cell viability is assessed using MTT or CellTiter-Glo assays. Antigen binding and internalization are measured by flow cytometry. These assays confirm the functional activity of the ADC. The linker itself is not tested in cell culture.
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| Animal Protocol |
In vivo animal experiments are not performed with Dibromomaleimide-C5-COOH itself. This compound is a synthetic building block used to construct ADCs. Once an ADC is synthesized, it may be tested in animal models, typically xenograft models in mice. Tumor-bearing mice are administered the ADC, and tumor growth inhibition, pharmacokinetics, and toxicity are evaluated. However, the intermediate itself is not administered to animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not applicable to Dibromomaleimide-C5-COOH as it is a linker for ADC synthesis. The compound is a solid and is stored at -20°C. Its molecular weight and formula are characterized. These properties are relevant for its use in chemical synthesis. No ADME studies are performed on this intermediate. Its stability in solution is assessed to ensure efficient conjugation. It is not intended for biological administration.
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| Toxicity/Toxicokinetics |
Toxicological data for Dibromomaleimide-C5-COOH are not available as it is a research chemical intermediate. Standard laboratory safety precautions for handling chemical reagents should be followed. The compound is not intended for human or animal consumption. Its specific toxicity profile has not been established. Any toxicological assessment would be performed on the final ADC drug candidate, not on this synthetic precursor. It is handled as a potentially hazardous material.
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| References | |
| Additional Infomation |
Dibromomaleimide-C5-COOH (DBM-C5-COOH) is a bifunctional dibromomaleimide linker used for bioconjugation and ADC synthesis. It is also known as Mal(Br2)-Aca. It can be used to connect MMAF and synthesize ADCs. It features a reactive dibromomaleimide group for thiol conjugation and a carboxylic acid for further functionalization. It is available for research use only.
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| Molecular Formula |
C10H11NO4BR2
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|---|---|
| Molecular Weight |
369.007
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| Exact Mass |
368.903
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| CAS # |
1443214-97-8
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| PubChem CID |
89614169
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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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 |
6
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| Heavy Atom Count |
17
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| Complexity |
368
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(CCC(=O)O)CCN1C(=O)C(=C(C1=O)Br)Br
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| InChi Key |
XABAXSUMIXSPEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11Br2NO4/c11-7-8(12)10(17)13(9(7)16)5-3-1-2-4-6(14)15/h1-5H2,(H,14,15)
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| Chemical Name |
6-(3,4-dibromo-2,5-dioxopyrrol-1-yl)hexanoic acid
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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 (~271.00 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7100 mL | 13.5498 mL | 27.0995 mL | |
| 5 mM | 0.5420 mL | 2.7100 mL | 5.4199 mL | |
| 10 mM | 0.2710 mL | 1.3550 mL | 2.7100 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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