| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
αvβ3
Cyclo(Arg-Gly-Asp-D-Phe-Cys) targets the αvβ3 integrin receptor, a cell surface receptor that plays a critical role in cell adhesion, migration, angiogenesis, and tumor progression. The RGD sequence is a specific recognition motif for integrins, and cyclic RGD peptides have high affinity and selectivity for αvβ3 integrin. By binding to αvβ3 integrin, cyclo(RGDfC) disrupts cell integrin interactions, inhibiting cell adhesion, migration, and angiogenesis. The compound's cyclic structure provides enhanced resistance to proteolytic degradation. |
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| ln Vitro |
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (0.5 mM; 24 h) reduces the expression of Oct 4, Sox 2, and Nanog, three mESC transcription factors [1]. Inhibiting integrin gene expression in the mESC-col I (type I collagen) construct is Cyclo(Arg-Gly-Asp-D-Phe-Cys) (0.5 mM) [1]. Cyclo(Arg-Gly-Asp-D-Phe-Cys) (0.5 mM) treatment caused mESCs to cluster and separate from the surface [1].
In vitro studies demonstrate that cyclo(RGDfC) is a high-affinity ligand for the αvβ3 integrin receptor. The compound inhibits the pluripotency gene expression of embryonic stem cells (ESCs). As a cyclic RGD peptide, it exhibits enhanced resistance to proteolytic degradation compared to linear RGD peptides. Cyclo(RGDfC) disrupts cell integrin interactions, inhibiting cell adhesion and migration. The compound is used in the study of cell adhesion and signaling pathways. |
| ln Vivo |
In either scenario, leukemia inhibitory factor (LIF) (injection in both legs) (SCID) mice treated with cyclo(Arg-Gly-Asp-D-Phe-Cys) (0.5 mM, 24 h)-treated mESCs do not cause teratomas, indicating that integrin interactions are necessary for the process of mESC tumor formation in vivo [1].
In vivo, cyclo(RGDfC) inhibits the tumorigenic potential of mouse embryonic stem cells (mESCs). The compound's ability to bind αvβ3 integrin and inhibit angiogenesis makes it a promising candidate for cancer therapy and imaging applications. The compound's cyclic structure provides enhanced stability in vivo. Further studies would be needed to evaluate its efficacy in various cancer models. |
| Enzyme Assay |
The binding of cyclo(RGDfC) to αvβ3 integrin can be assessed using surface plasmon resonance (SPR) or ELISA-based assays. In a typical SPR assay, recombinant αvβ3 integrin is immobilized on a sensor chip, and varying concentrations of cyclo(RGDfC) are injected over the surface. The association rate (ka), dissociation rate (kd), and equilibrium dissociation constant (KD) are calculated. The specificity of cyclo(RGDfC) for αvβ3 integrin over other integrins can be confirmed using similar assays.
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| Cell Assay |
RT-PCR[1]
Cell Types: MESCs Tested Concentrations: 0.5 mM Incubation Duration: 24 h Experimental Results: Down-regulated Oct 4, Nanog, Sox 2 by 99%, 97.5%, and 90% respectively. The cellular activity of cyclo(RGDfC) is assessed using cell-based assays. Cells expressing αvβ3 integrin are treated with varying concentrations of cyclo(RGDfC). Cell adhesion to integrin substrates is assessed using adhesion assays. Cell migration is assessed using wound healing or Transwell assays. Angiogenesis is assessed using endothelial cell tube formation assays. The compound's effects on pluripotency gene expression are assessed by qPCR or Western blotting. |
| Animal Protocol |
Cyclo(RGDfC) has been evaluated in animal models of cancer. In these studies, the compound inhibits the tumorigenic potential of mouse embryonic stem cells. The compound's ability to bind αvβ3 integrin and inhibit angiogenesis makes it a promising candidate for cancer therapy and imaging applications. Further studies would be needed to evaluate its efficacy in various cancer models.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for cyclo(RGDfC). The compound has a molecular weight of 578.64 and a molecular formula of C24H34N8O7S. As a cyclic peptide, it has enhanced resistance to proteolytic degradation compared to linear peptides. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties, including bioavailability, plasma protein binding, clearance, and half-life.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for cyclo(RGDfC). As a peptide that targets integrins, it may have on-target effects on normal tissues where integrins play important roles. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo(RGDfC), CAS# 862772-11-0) is a synthetic cyclic pentapeptide with high affinity for the αvβ3 integrin receptor. It exhibits enhanced resistance to proteolytic degradation compared to linear RGD peptides. Cyclo(RGDfC) inhibits pluripotency gene expression in ESCs and inhibits the tumorigenic potential of mESCs in vivo. The compound is used in the study of cell adhesion, migration, angiogenesis, and cancer. The molecular formula is C24H34N8O7S and molecular weight is 578.64.
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| Molecular Formula |
C24H34N8O7S
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|---|---|
| Molecular Weight |
578.64
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| Exact Mass |
578.227
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| CAS # |
862772-11-0
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| Related CAS # |
Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA
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| PubChem CID |
11330668
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| Appearance |
White to off-white solid powder
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| LogP |
-2.2
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
40
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| Complexity |
969
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCCN=C(N)N)CS)CC2=CC=CC=C2)CC(=O)O
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| InChi Key |
WNYJVAMZRBTOPE-YVSFHVDLSA-N
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| InChi Code |
InChI=1S/C24H34N8O7S/c25-24(26)27-8-4-7-14-20(36)28-11-18(33)29-16(10-19(34)35)22(38)31-15(9-13-5-2-1-3-6-13)21(37)32-17(12-40)23(39)30-14/h1-3,5-6,14-17,40H,4,7-12H2,(H,28,36)(H,29,33)(H,30,39)(H,31,38)(H,32,37)(H,34,35)(H4,25,26,27)/t14-,15+,16-,17-/m0/s1
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| Chemical Name |
2-[(2S,5R,8R,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-3,6,9,12,15-pentaoxo-8-(sulfanylmethyl)-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic 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 (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 : 50 mg/mL (86.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.32 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 25.0 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: ≥ 2.5 mg/mL (4.32 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7282 mL | 8.6410 mL | 17.2819 mL | |
| 5 mM | 0.3456 mL | 1.7282 mL | 3.4564 mL | |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7282 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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