| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Cleavable Linker
Mc-GGFG-OH targets cathepsin B, a cysteine protease that is overexpressed in the tumor microenvironment. The GGFG peptide sequence is a substrate for cathepsin B, which cleaves the peptide bond, releasing the cytotoxic payload specifically in cancer cells. This targeted release mechanism minimizes systemic toxicity and enhances the therapeutic index of the ADC. The Mc (maleimidocaproyl) group is used for conjugation to thiol groups on antibodies or other targeting ligands. Mc-GGFG-OH is a valuable tool for the development of targeted cancer therapies, including ADCs and PROTACs. |
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| ln Vitro |
In vitro studies on Mc-GGFG-OH are not typically performed on the linker itself, as it is a component of ADCs and PROTACs rather than a therapeutic agent. However, the linker's susceptibility to cleavage by cathepsin B can be assessed in vitro using purified cathepsin B or cell lysates. The release of the payload from the linker can be measured by HPLC or mass spectrometry. These assays are essential for characterizing the stability and release kinetics of ADCs and PROTACs containing the Mc-GGFG-OH linker. The compound is a valuable tool for the development of targeted cancer therapies.
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| ln Vivo |
In vivo studies on Mc-GGFG-OH are not typically performed on the linker itself, as it is a component of ADCs and PROTACs rather than a therapeutic agent. However, the linker's performance in vivo can be assessed as part of ADC or PROTAC studies. The selective release of the payload in the tumor microenvironment and the therapeutic efficacy of the ADC or PROTAC are evaluated in animal models of cancer. The Mc-GGFG-OH linker is a valuable tool for the development of targeted cancer therapies.
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| Enzyme Assay |
Non-cellular assays for Mc-GGFG-OH typically involve measuring the cleavage of the GGFG peptide sequence by purified cathepsin B or other proteases. The linker is incubated with the enzyme in a buffer system, and the cleavage products are analyzed by HPLC or mass spectrometry. The rate of cleavage and the specificity for cathepsin B can be determined. These assays are essential for characterizing the stability and release kinetics of ADCs and PROTACs containing the Mc-GGFG-OH linker. The compound's susceptibility to cleavage by other proteases can also be assessed to evaluate its selectivity.
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| Cell Assay |
In vitro cell-based assays for Mc-GGFG-OH are not typically performed on the linker itself, as it is a component of ADCs and PROTACs rather than a therapeutic agent. However, cell-based assays can be used to assess the activity of ADCs or PROTACs containing the Mc-GGFG-OH linker. These assays typically use cancer cell lines and measure cell viability, proliferation, or target protein degradation. The linker's ability to release the payload specifically in cancer cells can be assessed by comparing the activity of the ADC or PROTAC in cells that express cathepsin B versus those that do not.
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| Animal Protocol |
In vivo animal studies for Mc-GGFG-OH are not typically performed on the linker itself, as it is a component of ADCs and PROTACs rather than a therapeutic agent. However, animal studies can be used to assess the efficacy and safety of ADCs or PROTACs containing the Mc-GGFG-OH linker. These studies typically use mouse models of cancer and evaluate tumor growth inhibition, survival, and toxicity. The linker's ability to release the payload specifically in the tumor microenvironment and its contribution to the therapeutic index of the ADC or PROTAC are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Mc-GGFG-OH are not applicable, as the compound is a linker used in the synthesis of ADCs and PROTACs rather than a therapeutic agent. The pharmacokinetic properties of the linker are typically evaluated as part of the ADC or PROTAC. The linker's stability in plasma and its clearance are important factors for the performance of the ADC or PROTAC. However, specific PK data for Mc-GGFG-OH are not extensively documented in publicly available sources.
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| Additional Infomation |
Mc-GGFG-OH is a peptide linker used in ADC and PROTAC synthesis. It has the CAS number 2413428-36-9. The GGFG sequence is a cathepsin B substrate, enabling targeted payload release in tumors. Mc-GGFG-OH is not a drug and is strictly a research chemical for the development of targeted cancer therapies.
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| Molecular Formula |
C25H31N5O8
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|---|---|
| Molecular Weight |
529.54234623909
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| Exact Mass |
529.217
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| Elemental Analysis |
C, 56.70; H, 5.90; N, 13.23; O, 24.17
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| CAS # |
2413428-36-9
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| Related CAS # |
2413428-36-9;
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| PubChem CID |
153541851
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| Appearance |
White to yellow solid powder
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| LogP |
-0.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
38
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| Complexity |
911
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C(C=C1)C[C@@H](C(=O)NCC(=O)O)NC(=O)CNC(=O)CNC(=O)CCCCCN2C(=O)C=CC2=O
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| InChi Key |
DWPLKZYCOGLRPC-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C25H31N5O8/c31-19(9-5-2-6-12-30-22(34)10-11-23(30)35)26-14-20(32)27-15-21(33)29-18(25(38)28-16-24(36)37)13-17-7-3-1-4-8-17/h1,3-4,7-8,10-11,18H,2,5-6,9,12-16H2,(H,26,31)(H,27,32)(H,28,38)(H,29,33)(H,36,37)/t18-/m0/s1
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| Chemical Name |
(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl)glycylglycyl-L-phenylalanylglycine
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| Synonyms |
DSN28369; DSN-28369; DSN 28369
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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 : ~125 mg/mL (~236.05 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 | 1.8884 mL | 9.4422 mL | 18.8843 mL | |
| 5 mM | 0.3777 mL | 1.8884 mL | 3.7769 mL | |
| 10 mM | 0.1888 mL | 0.9442 mL | 1.8884 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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