| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Cleavable Linker
Mc-GGFG-PAB-OH TFA does not target a biological receptor; it serves as a chemical linker in antibody-drug conjugates (ADCs). Its tetrapeptide sequence (Gly-Gly-Phe-Gly) is specifically recognized and cleaved by cathepsin B, which is overexpressed in the lysosomes of many cancer cells. |
|---|---|
| ln Vitro |
ADC is made up of an antibody and an ADC linker that connects the cytotoxin to the antibody.
Not available. As an ADC linker, its in vitro activity is assessed via cleavage assays. The linker remains stable in circulation but undergoes proteolytic cleavage in the presence of cathepsin B, releasing the PAB spacer which spontaneously undergoes 1,6-elimination to liberate the attached cytotoxin. |
| ln Vivo |
Not available. As a linker component, the in vivo activity is evaluated when incorporated into a complete ADC conjugate. In xenograft models, ADCs containing Mc-GGFG-PAB linkers demonstrate targeted payload delivery and tumor growth inhibition with reduced systemic toxicity.
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| Enzyme Assay |
Not available. Standard cathepsin cleavage assays for this linker involve incubating the linker-payload conjugate (1-50 uM) with recombinant human cathepsin B (10-100 nM) in acetate buffer (pH 5.0-5.5, 50-100 mM) containing 2 mM DTT, at 37degC for 1-24 hours, followed by HPLC-MS analysis to quantify payload release.
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| Cell Assay |
Not available. For cellular internalization studies, typical protocols involve treating antigen-positive cancer cells with ADC conjugates containing this linker (0.01-10 nM) at 37degC for 4-24 hours, followed by lysis and analysis of released payload by LC-MS or assessment of cytotoxicity by viability assays.
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| Animal Protocol |
Not available. For in vivo studies of ADCs containing this linker, standard protocols involve intravenous administration of the ADC (1-20 mg/kg) in tumor-bearing mice, followed by serial blood collection to assess linker stability, tumor tissue collection to quantify payload release, and efficacy monitoring over 2-4 weeks.
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| ADME/Pharmacokinetics |
Not available. The pharmacokinetics of Mc-GGFG-PAB-based ADCs are primarily determined by the antibody component rather than the linker itself. The cathepsin-cleavable design provides stability in circulation (t1/2 days to weeks) with rapid cleavage upon lysosomal internalization.
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| Toxicity/Toxicokinetics |
Not available. Linkers themselves are generally non-toxic as they are not pharmacologically active; however, premature payload release due to linker instability can cause off-target toxicity. The cathepsin-cleavable mechanism is designed to minimize systemic toxicity while maximizing intratumoral activation.
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| Additional Infomation |
Mc-Gly-Gly-Phe-Gly-PAB-OH TFA is a research-grade cleavable ADC linker for the construction of antibody-drug conjugates. It has not been approved for clinical use. The TFA salt form improves solubility and handling characteristics. This product is exclusively for laboratory research in ADC development and targeted cancer therapy.
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| Molecular Formula |
C34H39F3N6O10
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|---|---|
| Related CAS # |
Mc-Gly-Gly-Phe-Gly-PAB-OH;2632342-05-1
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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: 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 :~250 mg/mL (~333.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (2.78 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
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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