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| Targets |
Cbz-D-Glu(Bn)-Gly-Gly-Gly-Gly does not bind to a specific biological target; it functions as a chemical linker in ADCs. The tetrapeptide sequence (glycine-rich) can be cleaved by specific proteases (e.g., cathepsins) in the lysosomal environment of target cells, enabling the release of a conjugated payload. It is a tool for bioconjugation rather than a drug.
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| ln Vitro |
As a cleavable ADC linker, Cbz-D-Glu(Bn)-Gly-Gly-Gly-Gly has no intrinsic in vitro activity. Its utility is demonstrated in ADC constructs where it is conjugated to a cytotoxic payload and an antibody. In cell-based assays, ADCs containing this linker show target-dependent cytotoxicity. The linker is stable in circulation but cleaved in lysosomes, releasing the payload.
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| ln Vivo |
Cbz-D-Glu(Bn)-Gly-Gly-Gly-Gly is not administered directly in animal studies. Instead, it is incorporated into a complete ADC. In mouse xenograft models, ADCs containing this linker show target-dependent antitumor efficacy, with the linker enabling payload release within tumor cells. It is not intended as a standalone therapeutic.
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| Enzyme Assay |
In vitro stability assays are performed by incubating the Cbz-D-Glu(Bn)-Gly-Gly-Gly-Gly linker or an ADC containing it in human plasma or lysosomal extracts at 37degC. Samples are collected at various time points (0-72 hours), and cleavage is analyzed by LC-MS/MS to quantify released payload or linker fragments. Cathepsin B is often used for enzymatic cleavage studies.
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| Cell Assay |
For ADC cytotoxicity assays, target-positive cancer cells (e.g., HER2-positive SK-BR-3 cells) are seeded in 96-well plates. Cells are treated with serial dilutions of ADC (containing the linker) for 72-96 hours. Cell viability is measured using a luminescent assay. Off-target toxicity is assessed using target-negative cells.
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| Animal Protocol |
For efficacy studies, female immunocompromised mice (e.g., nude or NSG mice, 6-8 weeks) are implanted subcutaneously with target-positive tumor cells. When tumors reach ~150-200 mm3, mice are randomized and treated intravenously with ADC (1-10 mg/kg, once weekly for 2-3 weeks) or vehicle. Tumor volumes are measured twice weekly for 3-4 weeks.
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| ADME/Pharmacokinetics |
Cbz-D-Glu(Bn)-Gly-Gly-Gly-Gly is not a drug and is not administered in vivo as a standalone entity. As a linker in ADCs, its pharmacokinetics are governed by the ADC itself. The linker is designed to be stable in circulation (pH 7.4, 37degC) but undergoes enzymatic cleavage upon internalization into lysosomes (pH ~4.5, containing cathepsins).
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| Toxicity/Toxicokinetics |
The Cbz and Bn protecting groups are generally considered non-toxic at the low concentrations encountered when the linker is used as part of an ADC. The linker itself is not administered directly. As a synthetic chemical intermediate, standard precautions for handling peptides and organic solvents apply (e.g., avoid inhalation, skin contact).
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| Additional Infomation |
Cbz-D-Glu(Bn)-Gly-Gly-Gly-Gly is a cleavable peptide linker classified as an ADC linker. It contains a Cbz protecting group for stability, a D-glutamic acid residue for branching, and a glycine-rich tetrapeptide sequence for enzyme recognition. Molecular weight is 599.59, and purity is ≥95%. It is stored at -20degC, protected from light.
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| Molecular Formula |
C28H33N5O10
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| Molecular Weight |
599.59
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| Appearance |
Typically exists as solid at room temperature
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6678 mL | 8.3390 mL | 16.6781 mL | |
| 5 mM | 0.3336 mL | 1.6678 mL | 3.3356 mL | |
| 10 mM | 0.1668 mL | 0.8339 mL | 1.6678 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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