| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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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 |
| Targets |
Cyclo(Phe-Gly) shows weak antagonistic activity against VEGFR2-CD (vascular endothelial growth factor receptor 2). It also exhibits strong inhibitory activity against human cancer cells (KB, KBv200) and has antimicrobial properties against various bacterial strains.
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|---|---|
| ln Vitro |
In cancer cell lines KB and KBv200, Cyclo(Phe-Gly) shows strong inhibitory activity with LD50 values of 6.5 and 11.2 umol/L, respectively. It inhibits VEGFR2-CD binding and exhibits antimicrobial activity against several bacterial strains, suggesting potential therapeutic applications.
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| ln Vivo |
In vivo activity data are limited. Cyclo(Phe-Gly) has been isolated from broth cultures of endophytic Streptomyces YIM 64018. Further in vivo studies in animal models are needed to evaluate its therapeutic potential and pharmacokinetic properties.
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| Enzyme Assay |
This cell-free assay is performed using purified VEGFR2-CD protein. Cyclo(Phe-Gly) (1-100 uM) is incubated with the protein in binding buffer for 1-2 hours. Binding affinity is measured by surface plasmon resonance (SPR) or fluorescence polarization. Antagonistic activity is assessed by measuring competition with a known VEGFR2 ligand.
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| Cell Assay |
KB and KBv200 human cancer cell lines are seeded in 96-well plates and treated with Cyclo(Phe-Gly) at varying concentrations (1-100 uM) for 48-72 hours. Cell viability is measured using MTT assay. LD50 values are calculated by fitting dose-response curves. For antimicrobial activity, bacterial strains (e.g., E. coli, S. aureus) are cultured and treated with Cyclo(Phe-Gly) to determine MIC values.
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| Animal Protocol |
Detailed animal protocols are not documented in available sources. Potential protocols for evaluating anti-tumor activity would involve establishing xenograft models with KB cells in nude mice, followed by intratumoral or systemic administration of Cyclo(Phe-Gly) at doses determined from in vitro LD50 values and pharmacokinetic data.
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| ADME/Pharmacokinetics |
Pharmacokinetic data are limited. Cyclo(Phe-Gly) is soluble in chloroform, dichloromethane, ethyl acetate, DMSO, and acetone. Storage: powder at -20degC, desiccated. Molecular weight: 204.23; formula: C11H12N2O2. Further PK studies are needed to determine bioavailability, half-life, and tissue distribution.
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| Toxicity/Toxicokinetics |
Standard safety precautions for research chemicals apply. Cyclo(Phe-Gly) is for research use only, not for human therapy. Avoid inhalation, ingestion, and skin contact. Use personal protective equipment and work in a well-ventilated area.
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| Additional Infomation |
This is a research-grade cyclic dipeptide, not an approved drug. It is found in nature (endophytic Streptomyces, Pantoea agglomerans) and serves as a lead compound for developing anticancer and antimicrobial agents. Purity: ≥98%. Also known as 3-benzylpiperazine-2,5-dione.
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| Molecular Formula |
C11H12N2O2
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|---|---|
| Molecular Weight |
204.225182533264
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| Exact Mass |
204.09
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| CAS # |
5037-75-2
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| PubChem CID |
138409
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| Appearance |
White to off-white solid powder
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| Density |
1.202g/cm3
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| Boiling Point |
535.1ºC at 760 mmHg
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| Flash Point |
242.8ºC
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| Index of Refraction |
1.555
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| LogP |
0.395
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
259
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C(CC2C=CC=CC=2)N([H])C(CN1[H])=O
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| InChi Key |
UZOJHXFWJFSFAI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12N2O2/c14-10-7-12-11(15)9(13-10)6-8-4-2-1-3-5-8/h1-5,9H,6-7H2,(H,12,15)(H,13,14)
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| Chemical Name |
3-benzylpiperazine-2,5-dione
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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 |
| 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 | 4.8964 mL | 24.4822 mL | 48.9644 mL | |
| 5 mM | 0.9793 mL | 4.8964 mL | 9.7929 mL | |
| 10 mM | 0.4896 mL | 2.4482 mL | 4.8964 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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