| 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 |
Tubulin
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| ln Vitro |
The MMAE component of this conjugate is a highly potent anti-tubulin agent. Upon cleavage of the peptide linker, MMAE is released and binds to tubulin, inhibiting its polymerization. This disrupts microtubule dynamics, leading to G2/M cell cycle arrest and subsequent apoptosis in target cells.
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| ln Vivo |
In vivo, the conjugate remains inactive until the antibody portion binds to a specific cancer cell surface antigen. Following internalization, the protease-cleavable linker is degraded, releasing MMAE selectively within the tumor microenvironment. This targeted delivery enhances efficacy and reduces systemic toxicity.
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| Enzyme Assay |
In a non-cell-based assay, the linker peptide (Ac-Lys-Val-Cit-PABC) is incubated with purified cathepsin B, a lysosomal protease that is often overexpressed in cancer cells. The reaction mixture is analyzed by HPLC-MS to monitor the release of the p-aminobenzyl carbamate (PABC) spacer. The efficiency of the enzyme-mediated cleavage is quantified to determine the enzymatic degradability of the linker.
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| Cell Assay |
For cell-based assays, cancer cells (e.g., HER2-positive breast cancer cells) are seeded in 96-well plates. After 24 hours, the cells are treated with various concentrations of the ADC or its cytotoxic payload for 48-72 hours. Cell viability is then assessed using a standard CCK-8 or MTT assay. IC50 values are calculated to evaluate the ADC's potency against the target cancer cells.
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| Animal Protocol |
In a typical xenograft model, immunodeficient mice are subcutaneously inoculated with human cancer cells (e.g., with EGFR expression). When the tumor reaches a certain size (e.g., 100-200 mm3), the mice are administered the ADC via intravenous injection. Tumor volumes and body weights are measured every 2-3 days. The tumor growth inhibition (TGI) rate is calculated at the end of the study.
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| ADME/Pharmacokinetics |
PK studies in rodents typically involve a single intravenous administration of the ADC. Blood samples are collected at various time points (e.g., 5 min, 30 min, 1, 2, 4, 8, 24, 48, 72, 96, 168 hours post-dose). Plasma concentrations of the total antibody, ADC, and released MMAE are quantified using ELISA and LC-MS/MS methods to determine key PK parameters like half-life, clearance, and exposure.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for this research linker-payload conjugate. The parent cytotoxic agent, MMAE, has well-documented toxicity, primarily neutropenia and peripheral neuropathy, which is common for microtubule inhibitors. Toxicity studies are typically performed on the final ADC construct, not the intermediate linker-payload.
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| References | |
| Additional Infomation |
This conjugate is a key intermediate in the development of ADCs. The Val-Cit-PABC linker is designed for cathepsin B cleavage, a feature used in FDA-approved ADCs like brentuximab vedotin (Adcetris®). MMAE is a synthetic antineoplastic agent that functions as a potent anti-mitotic toxin. This product is strictly for research purposes and is not a clinical drug.
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| Molecular Formula |
C67H110N12O16
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|---|---|
| Molecular Weight |
1339.66
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| Related CAS # |
Ac-Lys-Val-Cit-PABC-MMAE;1650569-89-3
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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 :~200 mg/mL (~149.29 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 | 0.7465 mL | 3.7323 mL | 7.4646 mL | |
| 5 mM | 0.1493 mL | 0.7465 mL | 1.4929 mL | |
| 10 mM | 0.0746 mL | 0.3732 mL | 0.7465 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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