| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
As a chemical linker for ADC construction, Val-Cit-PAB-OSBT does not have a defined biological target. Its role is to serve as a cleavable connector between an antibody and a cytotoxic payload in antibody-drug conjugates. The Val-Cit dipeptide is specifically cleaved by cathepsin B, enabling intracellular drug release. The OSBT group provides a handle for conjugation to the antibody.
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|---|---|
| ln Vitro |
In cell-free biochemical systems, this linker is used to synthesize antibody-drug conjugates. The Val-Cit-PAB sequence provides a cathepsin B-cleavable linkage that enables controlled drug release. The OSBT group reacts with functional groups on the antibody to form stable conjugates. The PAB spacer facilitates efficient payload release after enzymatic cleavage of the Val-Cit bond. The linker is a GMP-grade reagent.
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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. Antibody-drug conjugates constructed using this linker can be delivered to target cells where the antibody binds to cell surface antigens, followed by internalization into lysosomes. The Val-Cit dipeptide is cleaved by cathepsin B in the lysosomes, leading to the release of the cytotoxic payload. The self-immolative PAB group facilitates efficient payload release.
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| Enzyme Assay |
The cell-free assay for this linker involves conjugation reactions between the OSBT group and functional groups on antibodies. The reaction is typically performed in aqueous buffer under appropriate conditions. The efficiency of conjugation is assessed by mass spectrometry, SDS-PAGE, or HPLC analysis. The cleavability of the Val-Cit bond can be confirmed by treatment with cathepsin B enzyme, followed by analysis of payload release by HPLC or mass spectrometry.
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| Cell Assay |
No cell-based experimental protocols are directly applicable to this linker as it is a chemical synthesis reagent. Antibody-drug conjugates synthesized using this linker can be evaluated in cell culture experiments. Typical protocols include treating cancer cell lines expressing the target antigen with the ADC 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. The specificity of target cell killing is evaluated by comparing antigen-positive and antigen-negative cell lines.
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| Animal Protocol |
This linker is not administered to animals as it is a chemical intermediate for ADC synthesis. Antibody-drug conjugates incorporating this linker may be evaluated in animal models for pharmacokinetics and efficacy. Typical studies involve administration of the ADC 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 of ADC distribution, payload release, and therapeutic efficacy.
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| ADME/Pharmacokinetics |
As a chemical reagent, this compound does not have established pharmacokinetic properties. The pharmacokinetics of ADCs incorporating this linker depend on the antibody, payload, and overall conjugate properties. The cathepsin B-cleavable Val-Cit linker influences payload release kinetics in target cells. The compound itself is not intended for therapeutic use and is not administered systemically. The compound is typically stored at 4°C.
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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. Physical appearance is a solid. The compound is for research use only and is not for human therapeutic applications.
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| References | |
| Additional Infomation |
Val-Cit-PAB-OSBT is a research-grade chemical supplied for ADC linker synthesis applications. It is not an approved pharmaceutical and has no clinical trial history. The compound is a degradable ADC linker composed of the polypeptide Val-Cit-PAB and OSBT groups. Purity is typically 99.77%. This product is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C24N5O4SIH43
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|---|---|
| Molecular Weight |
493.7148
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| Exact Mass |
493.308
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| CAS # |
2210262-26-1
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| PubChem CID |
118703635
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
34
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| Complexity |
673
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| Defined Atom Stereocenter Count |
2
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| SMILES |
N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=O)C(NC1C=CC(CO[Si](C(C)(C)C)(C)C)=CC=1)=O)=O
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| InChi Key |
GFLUZYWIOXHYRH-PMACEKPBSA-N
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| InChi Code |
InChI=1S/C24H43N5O4Si/c1-16(2)20(25)22(31)29-19(9-8-14-27-23(26)32)21(30)28-18-12-10-17(11-13-18)15-33-34(6,7)24(3,4)5/h10-13,16,19-20H,8-9,14-15,25H2,1-7H3,(H,28,30)(H,29,31)(H3,26,27,32)/t19-,20-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-N-[4-[[tert-butyl(dimethyl)silyl]oxymethyl]phenyl]-5-(carbamoylamino)pentanamide
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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. |
| 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: ~300 mg/mL (~607.6 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (15.19 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 DMSO stock solution (75.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume 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: ≥ 7.5 mg/mL (15.19 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 DMSO stock solution (75.0 mg/mL) to 900 μL of 20% SBE-β-CD saline 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. Solubility in Formulation 3: ≥ 7.5 mg/mL (15.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (75.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0255 mL | 10.1274 mL | 20.2548 mL | |
| 5 mM | 0.4051 mL | 2.0255 mL | 4.0510 mL | |
| 10 mM | 0.2025 mL | 1.0127 mL | 2.0255 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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