| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
This compound does not target a biological receptor. It functions as a structural component in ADCs, acting as a protease-cleavable linker that is specifically recognized and cleaved by cathepsin B enzymes within lysosomes, facilitating targeted drug release.
|
|---|---|
| ln Vitro |
In vitro, Gly-Gly-Phe-Gly functions as an enzymatically cleavable peptide spacer. Studies have shown its utility in doxorubicin (DXR) conjugates, where controlled drug release is achieved by enzymatic hydrolysis, enhancing cytotoxicity in target cells.
|
| ln Vivo |
No direct in vivo activity is attributed to the peptide alone. However, when incorporated into ADCs such as Puxitatug samrotecan (AZD8205), it contributes to the conjugate's in vivo antitumor efficacy by releasing the cytotoxic payload within the tumor microenvironment.
|
| Enzyme Assay |
Not specified for the unconjugated peptide. Standard protocols for evaluating peptide linkers involve cathepsin B cleavage assays. The peptide is incubated with the enzyme, and cleavage products are analyzed by HPLC or LC-MS to measure hydrolysis kinetics.
|
| Cell Assay |
Not specified for the peptide alone. Standard cell-based assays for ADC linkers involve treating antigen-positive cancer cells with the ADC. The peptide's cleavability is inferred from the potency of the ADC (IC50 values) and by measuring released payload in lysates using LC-MS.
|
| Animal Protocol |
Not applicable for the peptide alone. For ADC candidates incorporating this linker, in vivo efficacy is typically assessed in murine xenograft models. The ADC is administered intravenously (e.g., 1-10 mg/kg), and tumor volume inhibition is monitored over 2-4 weeks.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data are not available for the isolated peptide. For ADC linkers, stability in plasma is critical; the GGFG linker demonstrates good plasma stability and controlled intracellular release, avoiding premature payload release in circulation.
|
| Toxicity/Toxicokinetics |
As a research-grade chemical, Gly-Gly-Phe-Gly is considered non-toxic at standard usage concentrations. In ADC applications, the linker itself does not contribute to toxicity; the safety profile is determined by the conjugated payload and the targeting antibody.
|
| References |
[1]. Shiose Y, et al. Systematic research of peptide spacers controlling drug release from macromolecular prodrug system, carboxymethyldextran polyalcohol-peptide-drug conjugates. Bioconjug Chem. 2009 Jan;20(1):60-70.
|
| Additional Infomation |
This tetrapeptide is a research tool used as an ADC linker or peptide spacer. It is featured in ADC products like Puxitatug samrotecan (AZD8205) and has been applied to doxorubicin conjugates. It has no approved status as a standalone drug.
|
| Molecular Formula |
C15H20N4O5
|
|---|---|
| Molecular Weight |
336.34
|
| Exact Mass |
336.143
|
| CAS # |
200427-88-9
|
| PubChem CID |
9945687
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.21
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
24
|
| Complexity |
463
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1=CC=C(C=C1)CC(C(=O)NCC(=O)O)NC(=O)CNC(=O)CN
|
| InChi Key |
HXUVTXPOZRFMOY-NSHDSACASA-N
|
| InChi Code |
InChI=1S/C15H20N4O5/c16-7-12(20)17-8-13(21)19-11(15(24)18-9-14(22)23)6-10-4-2-1-3-5-10/h1-5,11H,6-9,16H2,(H,17,20)(H,18,24)(H,19,21)(H,22,23)/t11-/m0/s1
|
| Chemical Name |
2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]acetic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (297.32 mM)
|
|---|---|
| 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 | 2.9732 mL | 14.8659 mL | 29.7318 mL | |
| 5 mM | 0.5946 mL | 2.9732 mL | 5.9464 mL | |
| 10 mM | 0.2973 mL | 1.4866 mL | 2.9732 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
