| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Cys-mc-MMAE targets microtubules through its MMAE payload. MMAE is a potent antimitotic agent that inhibits tubulin polymerization, leading to cell cycle arrest and apoptosis. The non-cleavable maleimidocaproyl linker provides stability to the ADC, while the cysteine moiety alters the physicochemical properties of the final conjugate. Unlike cleavable linkers, the non-cleavable mc linker releases the MMAE payload only after internalization and lysosomal degradation of the ADC.
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| ln Vitro |
In vitro, Cys-mc-MMAE is used to synthesize ADCs that demonstrate potent cytotoxicity against antigen-positive cancer cells. The ionized cysteine moiety in Cys-mc-MMAE alters the physicochemical and pharmacological properties of the final ADC, directly influencing parameters such as bystander effect, permeability, and conjugation site specificity. ADCs synthesized with this linker-payload show optimal therapeutic safety profiles. The MMAE payload inhibits tubulin polymerization, leading to potent antimitotic activity.
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| ln Vivo |
In vivo, ADCs synthesized using Cys-mc-MMAE demonstrate antitumor efficacy in preclinical models. The non-cleavable linker provides stability in circulation, reducing premature payload release and off-target toxicity. The ionized cysteine moiety may influence the pharmacokinetic and biodistribution properties of the ADC. Detailed in vivo efficacy data, including tumor growth inhibition and survival benefits in xenograft models, are described in the primary literature.
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| Enzyme Assay |
Non-cellular assays for Cys-mc-MMAE involve characterizing its conjugation to antibodies. The maleimide group reacts with reduced cysteine residues on antibodies to form stable thioether bonds. Conjugation efficiency and drug-to-antibody ratio (DAR) are assessed by HPLC, mass spectrometry, or hydrophobic interaction chromatography (HIC). The stability of the conjugate in plasma and its aggregation propensity are evaluated. The MMAE payload's activity can be confirmed in tubulin polymerization assays.
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| Cell Assay |
In vitro cellular experiments using Cys-mc-MMAE-based ADCs are conducted in antigen-positive and antigen-negative cancer cell lines. Cells are treated with the ADC at various concentrations, and cell viability is assessed using CellTiter-Glo or MTT assays. The specificity of cytotoxicity is confirmed by comparing antigen-positive versus antigen-negative cells. Cellular uptake and intracellular trafficking are assessed by fluorescence microscopy or flow cytometry. Apoptosis induction is evaluated by caspase activity or Annexin V staining.
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| Animal Protocol |
In vivo animal studies using Cys-mc-MMAE-based ADCs are performed in murine xenograft models using antigen-positive cancer cell lines. Tumor-bearing mice are treated with the ADC via intravenous administration. Tumor growth is monitored over time, and endpoints include tumor volume measurements, survival analysis, and pharmacokinetic assessments. The therapeutic window and safety profile of the ADC are evaluated by monitoring body weight and clinical signs.
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| ADME/Pharmacokinetics |
Cys-mc-MMAE has a molecular formula of C52H85N7O12S and a molecular weight of 1032.3 g/mol. The compound is stored according to the manufacturer's recommendations, typically at -20°C protected from light. It is soluble in DMSO and other organic solvents suitable for bioconjugation reactions. The compound is for research use only and is used in the synthesis of ADCs. Purity is typically ≥95%.
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| Toxicity/Toxicokinetics |
Toxicity data for Cys-mc-MMAE are evaluated as part of the safety assessment of ADCs synthesized using this linker-payload. The MMAE payload is a potent antimitotic agent and can cause on-target off-tumor toxicity if not properly targeted. The non-cleavable linker helps to reduce premature payload release, improving the safety profile of the ADC. Standard toxicology studies assess the safety of the final ADC. The compound itself is for research use only.
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| References | |
| Additional Infomation |
Cys-mc-MMAE is a drug-linker conjugate for ADC synthesis. A key reference is Wang Y, et al. "Antibody-Drug Conjugate Using Ionized Cys-Linker-MMAE as the Potent Payload Shows Optimal Therapeutic Safety." Cancers (Basel). 2020. The ionized cysteine moiety distinguishes this conjugate from standard cleavable linker-payloads such as MC-VC-PAB-MMAE. All products are for research use only.
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| Molecular Formula |
C52H85N7O12S
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| Molecular Weight |
1032.34
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| Appearance |
White to off-white solid powder
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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 :~100 mg/mL (~96.87 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.42 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 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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 (2.42 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.42 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 | 0.9687 mL | 4.8434 mL | 9.6867 mL | |
| 5 mM | 0.1937 mL | 0.9687 mL | 1.9373 mL | |
| 10 mM | 0.0969 mL | 0.4843 mL | 0.9687 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.
Products are for research use only; We do not sell to patients
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