| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
Mal-C5-N-bis(PEG2-C2-acid) does not target biological receptors; it is a chemical linker used in ADC construction. The branched structure allows two payload molecules to be attached per linker, potentially increasing the drug-to-antibody ratio (DAR) and therapeutic potency while maintaining favorable physicochemical properties.
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| ln Vitro |
Not available. As an ADC linker, its activity is evaluated when incorporated into ADCs with dual payloads. The branched PEG2 arms provide solubility and flexibility, potentially allowing two distinct payloads or two copies of the same payload, which may enhance potency or enable combination effects from a single ADC.
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| ln Vivo |
Not available. ADCs constructed with Mal-C5-N-bis(PEG2-C2-acid) linkers have potential for enhanced efficacy in mouse xenograft models due to increased DAR. The branched PEG architecture may improve pharmacokinetics and reduce aggregation compared to linear linkers at high DAR. Specific in vivo data for this linker are not available.
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| Enzyme Assay |
Not available. Standard maleimide-thiol conjugation assays involve incubating Mal-C5-N-bis(PEG2-C2-acid) with reduced antibody thiols (e.g., generated by TCEP reduction of interchain disulfides) at pH 6.5-7.5 for 2-4 hours at 4degC or room temperature, followed by purification by size exclusion chromatography. Conjugation efficiency is assessed by MALDI-TOF or HIC-HPLC.
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| Cell Assay |
Not available. For ADC activity assessment, typical protocols involve treating antigen-positive cancer cells with dual-payload ADCs (0.001-100 nM) for 72-120 hours, followed by viability assays. The dual payload design may produce enhanced cytotoxicity or overcome resistance mechanisms compared to single-payload ADCs.
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| Animal Protocol |
Not available. For in vivo studies, standard protocols involve intravenous administration of dual-payload ADCs (1-30 mg/kg) in tumor-bearing mice, monitoring tumor volume for 4-6 weeks. Pharmacokinetic studies assess stability of the maleimide linkage (prone to reverse thiol exchange in circulation) and payload release kinetics.
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| ADME/Pharmacokinetics |
The maleimide-C5-PEG2-acid linker provides improved aqueous solubility compared to purely hydrophobic linkers. The C5 spacer reduces steric hindrance. However, maleimide linkages are susceptible to reverse thiol exchange in circulation (retro-Michael reaction), leading to payload loss. Branched PEG2 arms enhance solubility and stability.
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| Toxicity/Toxicokinetics |
Maleimide-antibody conjugates can undergo deconjugation via retro-Michael reaction, releasing free payload into circulation and potentially increasing systemic toxicity. The PEG2 arms reduce this risk by shielding the maleimide group. Specific toxicological data for this linker are not reported.
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| References |
[1]. Mark Frigerio, et al. The Chemical Design and Synthesis of Linkers Used in Antibody Drug Conjugates. Curr Top Med Chem. 2017;17(32):3393-3424.
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| Additional Infomation |
Mal-C5-N-bis(PEG2-C2-acid) is a research-grade branched ADC linker designed for dual payload conjugation and enhanced solubility. It has not entered clinical trials nor been approved for therapeutic use. This product is for laboratory research in ADC development, enabling exploration of high-DAR and dual-payload strategies for targeted cancer therapy.
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| Molecular Formula |
C24H38N2O11
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|---|---|
| Appearance |
Colorless to light yellow viscous liquid
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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) |
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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