| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
As a chemical linker for ADC synthesis, diMal-O-CH2COOH does not have a defined biological target. Its role is to serve as a cleavable connector between biomolecules. The two maleimide groups enable conjugation to thiol groups on antibodies or other proteins, while the carboxylic acid provides a handle for payload attachment. The cleavable nature of the linker enables controlled release in the target environment.
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| ln Vitro |
In cell-free biochemical systems, this linker is used to synthesize bioconjugates, including ADCs, protein-protein crosslinks, and surface modifications. The maleimide groups react with thiol groups on proteins or antibodies to form stable thioether bonds. The carboxylic acid can be activated for payload attachment using EDC or HATU. The cleavable nature of the linker enables controlled release.
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| ln Vivo |
This compound does not exhibit direct cellular activity as it is a chemical linker rather than a bioactive molecule. Bioconjugates constructed using this linker can be delivered to target cells where the antibody binds to cell surface antigens, followed by internalization. The cleavable nature of the linker enables controlled release of the payload within target cells.
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| Enzyme Assay |
The cell-free assay for this linker involves conjugation reactions between the maleimide groups and thiol groups on proteins, and between the carboxylic acid and amines on payloads. The maleimide-thiol reaction is typically performed in aqueous buffer at pH 6.5-7.5 for 1-4 hours at room temperature or 4°C. The carboxylic acid can be activated for payload attachment. The efficiency of conjugation is assessed by mass spectrometry, SDS-PAGE, or HPLC analysis.
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| Cell Assay |
No cell-based experimental protocols are directly applicable to this linker as it is a chemical synthesis reagent. Bioconjugates synthesized using this linker can be evaluated in cell culture experiments. Typical protocols include treating cancer cell lines with the conjugate at concentrations ranging from 0.001 to 10 μg/mL. Cells are incubated for 24-96 hours, and cell viability is assessed using MTT or CCK-8 assays.
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| Animal Protocol |
This linker is not administered to animals as it is a chemical intermediate for bioconjugate synthesis. Bioconjugates incorporating this linker may be evaluated in animal models for pharmacokinetics and efficacy. Typical studies involve administration of the conjugate to tumor-bearing mice via intravenous routes at doses ranging from 0.1-10 mg/kg. Tumor volumes are measured, and tissues are collected for analysis.
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| ADME/Pharmacokinetics |
As a chemical reagent, this compound does not have established pharmacokinetic properties. The pharmacokinetics of bioconjugates incorporating this linker depend on the biomolecule, payload, and overall conjugate properties. The cleavable nature of the linker influences payload release kinetics. The compound itself is not intended for therapeutic use.
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| Toxicity/Toxicokinetics |
The compound is not intended for therapeutic use and lacks established toxicity profiles. Standard laboratory safety precautions should be observed when handling this chemical reagent. The compound is typically stored at 4°C, protected from light. It is for research use only and is not for human therapeutic applications.
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| Additional Infomation |
diMal-O-CH2COOH is a research-grade chemical supplied for ADC and bioconjugation applications. It is not an approved pharmaceutical and has no clinical trial history. The compound is a cleavable bismaleimide ADC linker. This product is intended for research use only.
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| Molecular Formula |
C13H12N2O7
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|---|---|
| Exact Mass |
308.064
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| CAS # |
1620837-47-9
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| PubChem CID |
77106253
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
528
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=O)N(C1=O)CC(CN2C(=O)C=CC2=O)OCC(=O)O
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| InChi Key |
JREDLPVQALHAIP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12N2O7/c16-9-1-2-10(17)14(9)5-8(22-7-13(20)21)6-15-11(18)3-4-12(15)19/h1-4,8H,5-7H2,(H,20,21)
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| Chemical Name |
2-[1,3-bis(2,5-dioxopyrrol-1-yl)propan-2-yloxy]acetic 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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
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.
Products are for research use only; We do not sell to patients
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