| 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 |
Auristatin
Tubulin (via MMAE payload). MMAE is a potent tubulin inhibitor that binds to the tubulin protein, preventing microtubule polymerization and causing G2/M cell cycle arrest and apoptosis. The SuO-Val-Cit-PAB linker is cleaved by lysosomal proteases (cathepsin B) upon internalization into cancer cells, releasing the active MMAE payload. |
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| ln Vitro |
ADCs are made up of an antibody and an ADC cytotoxin that are joined together by an ADC linker.
SuO-Val-Cit-PAB-MMAE is not tested directly in vitro for activity, as it is a linker-payload conjugate intended for ADC synthesis. The MMAE payload itself potently inhibits tubulin polymerization and kills cancer cells with IC50 values in the low picomolar to nanomolar range. The Val-Cit linker is stable in circulation but is efficiently cleaved by cathepsin B in lysosomes. |
| ln Vivo |
In vivo, when conjugated to a tumor-specific antibody, the resulting ADC is internalized by target cancer cells, and the SuO-Val-Cit-PAB linker is cleaved in lysosomes, releasing MMAE. This leads to potent and selective tumor growth inhibition with reduced systemic toxicity compared to unconjugated MMAE. The Val-Cit linker provides a good balance of stability and cleavability.
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| Enzyme Assay |
Cathepsin B cleavage assay: SuO-Val-Cit-PAB-MMAE is incubated with recombinant cathepsin B (10 nM) in cleavage buffer (100 mM sodium acetate, pH 5.5, 2 mM DTT, 2 mM EDTA) at 37degC for 0-24 h. The reaction is stopped by adding E-64 protease inhibitor. The amount of released MMAE is quantified by HPLC-MS/MS. Cleavage efficiency is calculated as the percentage of free MMAE generated over total linker-payload.
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| Cell Assay |
ADC internalization and cytotoxicity assay: Target-positive cancer cells are seeded in 96-well plates and treated with an ADC synthesized using SuO-Val-Cit-PAB-MMAE (0-100 nM, 72 h). Alternatively, a dummy antibody is used for non-targeting control. Cell viability is assessed by CCK-8 or MTT. For internalization, cells are treated with fluorescently labeled ADC and imaged by confocal microscopy.
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| Animal Protocol |
Xenograft tumor model: Mice bearing target antigen-positive tumor xenografts are treated with an ADC synthesized using SuO-Val-Cit-PAB-MMAE (1-10 mg/kg, i.v., once weekly for 2-3 weeks). Tumor volume is measured twice weekly. At study termination, tumors are collected for immunohistochemistry (cleaved caspase-3, Ki-67). Plasma MMAE levels are measured by LC-MS/MS to assess linker stability in circulation.
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| ADME/Pharmacokinetics |
For ADCs bearing the SuO-Val-Cit-PAB-MMAE payload, the linker-payload conjugate is stable in circulation (half-life of 2-4 days in humans and 1-3 days in rodents) but is rapidly cleaved upon lysosomal internalization. The MMAE payload has a short plasma half-life once released (minutes to hours). The molecular weight of the conjugate is 1264.51, and it is soluble in DMSO (50 mg/mL).
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| Toxicity/Toxicokinetics |
Toxicity data for the SuO-Val-Cit-PAB-MMAE linker-payload itself are limited, as it is not administered as a standalone therapeutic. When conjugated to an antibody, ADC toxicity profiles are typically driven by the payload and target expression. MMAE is associated with neutropenia and peripheral neuropathy. The Val-Cit linker has a clean preclinical toxicity profile. It is for research use only.
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| References | |
| Additional Infomation |
SuO-Val-Cit-PAB-MMAE is a research-grade drug-linker conjugate for ADC development and is not a finished drug product. It has not been approved for human therapeutic use. The Val-Cit-PAB (valine-citrulline-p-aminobenzyloxycarbonyl) linker is one of the most commonly used cleavable linkers in ADC design. The product should be stored at -80degC under nitrogen and used immediately after reconstitution.
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| Molecular Formula |
C63H97N11O16
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| Molecular Weight |
1264.51
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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: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 :~10 mg/mL (~7.91 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 | 0.7908 mL | 3.9541 mL | 7.9082 mL | |
| 5 mM | 0.1582 mL | 0.7908 mL | 1.5816 mL | |
| 10 mM | 0.0791 mL | 0.3954 mL | 0.7908 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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