| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA targets integrins, particularly alphavbeta3 and alphavbeta5. Integrins are cell surface receptors that mediate cell adhesion to the extracellular matrix and play crucial roles in cell migration, proliferation, and survival. As a cyclic RGD peptide, cRGDfV competitively binds to integrins, blocking their interaction with extracellular matrix proteins. This inhibits cell adhesion, migration, and angiogenesis. The compound's antitumor activity is attributed to its ability to inhibit integrin-mediated signaling in cancer cells.
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| ln Vitro |
Cyclo (Arg-Gly-Asp-D-Phe-Val) (TFA) (c (RGDfV)) (35 nM, 4–24 h) stops tumor cells from adhering to the substrate and from migrating, which causes blank cells to escape the protective layer.
In vitro, Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA functions as an integrin alphavbeta3 and alphavbeta5 antagonist. The compound competitively binds integrins to block their interaction with extracellular matrix proteins, thereby inhibiting cell adhesion, migration, and angiogenesis. The compound has antitumor activity. These in vitro properties establish Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA as a valuable tool for studying integrin biology and for therapeutic applications in cancer and angiogenesis-related disorders. |
| ln Vivo |
In vivo, Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA has been studied for its antitumor activity. The compound can be used for the research of acute myeloid leukemia. By inhibiting integrin-mediated cell adhesion, migration, and angiogenesis, the compound may suppress tumor growth and metastasis. Detailed in vivo efficacy data are available in the scientific literature. Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA is for research purposes only.
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| Enzyme Assay |
Receptor binding assays for Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA are performed using purified recombinant integrin proteins (alphavbeta3 or alphavbeta5) or using cell-based adhesion assays. Binding affinity is assessed using methods such as surface plasmon resonance (SPR), ELISA, or competition binding assays with labeled RGD peptides. The compound is incubated with the integrin protein at varying concentrations, and binding is measured. IC50 or Ki values are calculated from concentration-response curves. Nonspecific binding is determined in control reactions without competitor.
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: MV4-11 cells Tested Concentrations: 35 nM Incubation Duration: 24 h Experimental Results: Affects the leukemia cell cycle and decreases. The G0/G1 phase of leukemia cells increased in 3D and 2D culture systems, and the S phase of leukemia cells increased in 3D and 2D culture systems. Apoptosis analysis[1] Cell Types: MV4-11 Cell Tested Concentrations: 35 nM Incubation Duration: 24 hrs (hours) Experimental Results: Increased apoptosis rate. Cellular assays for Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA are performed using cancer cell lines that express integrins, such as melanoma or glioblastoma cells. Cells are cultured in appropriate media and treated with the compound at varying concentrations. Cell adhesion to extracellular matrix proteins (e.g., vitronectin, fibronectin) is assessed using adhesion assays. Cell migration is assessed using wound healing or Boyden chamber assays. Cell proliferation and angiogenesis are assessed using standard assays. The compound is typically dissolved in DMSO or water and diluted in cell culture media for treatment. |
| Animal Protocol |
In vivo studies with Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA are conducted in mouse xenograft models of cancer, including acute myeloid leukemia models. The compound is administered via appropriate routes (e.g., intravenous or intraperitoneal) at defined doses and schedules. Tumor growth is monitored by caliper measurements, and tumor volumes are calculated. Angiogenesis is assessed by measuring microvessel density in tumor tissues. Pharmacokinetic parameters are determined from plasma samples collected at various time points.
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| ADME/Pharmacokinetics |
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA has a molecular weight of 688.65 and a molecular formula of C29H43N9O8·C2HF3O2. The compound is a cyclic RGD peptide that acts as an integrin alphavbeta3 and alphavbeta5 antagonist. Detailed pharmacokinetic data for Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA are not extensively documented in publicly available literature. The compound is soluble in DMSO and water. It should be stored at -20degC.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA are not extensively documented in publicly available sources. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety and chemical hygiene guidelines. The compound has a purity of ≥98%.
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| References | |
| Additional Infomation |
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA (cRGDfV) is a cyclic RGD peptide that acts as an integrin (particularly alphavbeta3 and alphavbeta5) antagonist. It competitively binds integrins to block their interaction with extracellular matrix proteins, inhibiting cell adhesion, migration, and angiogenesis. The compound has antitumor activity and can be used for the research of acute myeloid leukemia. Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA is for research purposes only.
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| Molecular Formula |
C28H39F3N8O9
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|---|---|
| Molecular Weight |
688.652676820755
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| Exact Mass |
688.279
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| CAS # |
199807-33-5
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| Related CAS # |
Cyclo(Arg-Gly-Asp-D-Phe-Val);137813-35-5
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| PubChem CID |
131698036
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
48
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](C(=O)N1)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N.C(=O)(C(F)(F)F)O
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| InChi Key |
DEDCWVTYYHSZET-JDNDSRKHSA-N
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| InChi Code |
InChI=1S/C26H38N8O7.C2HF3O2/c1-14(2)21-25(41)32-16(9-6-10-29-26(27)28)22(38)30-13-19(35)31-18(12-20(36)37)23(39)33-17(24(40)34-21)11-15-7-4-3-5-8-15;3-2(4,5)1(6)7/h3-5,7-8,14,16-18,21H,6,9-13H2,1-2H3,(H,30,38)(H,31,35)(H,32,41)(H,33,39)(H,34,40)(H,36,37)(H4,27,28,29);(H,6,7)/t16-,17+,18-,21-;/m0./s1
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| Chemical Name |
2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid;2,2,2-trifluoroacetic acid
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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, 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) |
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 | 1.4521 mL | 7.2606 mL | 14.5212 mL | |
| 5 mM | 0.2904 mL | 1.4521 mL | 2.9042 mL | |
| 10 mM | 0.1452 mL | 0.7261 mL | 1.4521 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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