Cyclo(-RGDfK) TFA
Based on 31 publication(s) in Google Scholar
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 500577-51-5
- Formula: C29H42F3N9O9
- Molecular Weight:717.69
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cyclo(-RGDfK) TFA
More- Mater Today. 2026 Jan 7;92:453-472.
- Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]
- Bone Res. 2024 Aug 28;12(1):49. [Abstract]
- Acta Pharm Sin B. 2026 Jun 8.
- J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]
- Adv Sci (Weinh). 2026 Jun;13(33):e20635. [Abstract]
- Adv Sci (Weinh). 2025 Oct 30:e01602. [Abstract]
- J Nanobiotechnology. 2024 Sep 1;22(1):528. [Abstract]
- Engineering. 8 October 2020.
- EBioMedicine. 2026 Mar:125:106187. [Abstract]
- Adv Healthc Mater. 2021 Jul;10(13):e2100304. [Abstract]
- Acta Biomater. 2021 May:126:183-198. [Abstract]
- Free Radic Biol Med. 2024 Dec 9:227:296-311. [Abstract]
- Mater Today Nano. 2023 Dec:24:100432. [Abstract]
- ACS Appl Mater Interfaces. 2019 Jul 31;11(30):26648-26663. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2025 May 29:101548. [Abstract]
- Antioxidants (Basel). 2024 Nov 1;13(11):1339. [Abstract]
- Mol Ther Nucleic Acids. 2021 Jan 9;23:797-810. [Abstract]
- Drug Deliv Transl Res. 2024 Oct;14(10):2629-2641. [Abstract]
- ACS Biomater Sci Eng. 2023 May 8;9(5):2524-2533. [Abstract]
- Int Immunopharmacol. 2025 May 26:159:114947. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Mar 31;1871(5):167814. [Abstract]
- Heliyon. 2024 Jul 2;10(13):e34006. [Abstract]
- Mol Biol Rep. 2025 Feb 5;52(1):205. [Abstract]
- J Radiat Res Appl Sci. 2026 Mar 28.
- Biochem Biophys Res Commun. 2023 Sep 3:671:124-131. [Abstract]
- bioRxiv. 2026 Jun 25.
- SSRN. 2026 Mar 27.
- bioRxiv. 2025 April 01.
- Res Sq. 2024 Aug 07.
- bioRxiv. 2024 July 13.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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WB
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In Vivo Efficacy Study
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Cell Migration/Invasion Assay
Biological Activity
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αvβ3 0.94 nM (IC50) |
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin and exhibits a IC50 of 0.94 nM[1].[66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 500577-51-5
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Appearance Solid
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Molecular Weight 717.69
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Formula C29H42F3N9O9
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Color White to off-white
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Sequence
Cyclo(Arg-Gly-Asp-{dPhe}-Lys)
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Sequence Shortening
Cyclo(RGD-{dPhe}-K)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (31)
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Journal Impact Factor
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Most Recent
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Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: Mater Today. 2026 Jan 7;92:453-472.
Cyclo(-RGDfK) (200 μM; 1 h; 37 ℃) significantly reduced intracellular fluorescence intensity, indicating that the constructed LNP-RGD nanoparticles achieved efficient and targeted cellular uptake through RGD–integrin αvβ3 interactions.
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Bioact Mater
Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering. [Abstract]2021 Jan 7;6(7):2039-2057. PMID: 33511306
Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]
The integrin αvβ3 inhibitor Cyclo(-RGDfK) (20 μM; 1 h) significantly inhibited MSC migration.
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Bone Res
2024 Aug 28;12(1):49. PMID: 39198395 -
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J Extracell Vesicles
Exomeres From Adventitial Fibroblasts of Spontaneously Hypertensive Rats Promote Vascular Remodelling via Transferring Osteopontin. [Abstract]2025 Aug;14(8):e70146. PMID: 40767027
Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]
Integrin αVβ3 inhibitor Cyclo(-RGDfK) (10 μM) pretreatment prevented the S-EMs-induced proliferation of WKY and SHR 24 h after the application of the S-EMs.
Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]
Integrin αVβ3 inhibitor Cyclo(-RGDfK) (10 μM) prevented the increased ratios of P-PI3K/PI3K, P-AKT/AKT, and P-FAK/FAK in VSMCs of WKY and SHR that were promoted by S-EMs.
Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]
Cyclo (-RGDfK) (10 mg/kg; i.p.; every 2 d for 10 times) almost abolished vascular remodelling induced by S-EMs in the aorta of WKY mice.
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Adv Sci (Weinh)
Legumain Restrains Granuloma Formation by Inhibiting mTORC1/STAT1-Mediated M1 Macrophage Polarization in Sarcoidosis. [Abstract]2026 Jun;13(33):e20635. PMID: 41933939 -
Adv Sci (Weinh)
Cancer Immunotherapy via Disruption of Integrin αvβ3 and CD47 Costabilization on Cancer Cell Surface. [Abstract]2025 Oct 30:e01602. PMID: 41168993 -
J Nanobiotechnology
Aminolysis-mediated single-step surface functionalization of poly (butyl cyanoacrylate) microbubbles for ultrasound molecular imaging. [Abstract]2024 Sep 1;22(1):528. PMID: 39218888 -
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EBioMedicine
Parvimonas micra exacerbates periodontitis by infiltrating host cells through TmpC and circumventing lysosomal elimination via AppA. [Abstract]2026 Mar:125:106187. PMID: 41740230 -
Adv Healthc Mater
Enhanced Antitumor Efficacy through an "AND gate" Reactive Oxygen-Species-Dependent pH-Responsive Nanomedicine Approach. [Abstract]2021 Jul;10(13):e2100304. PMID: 34050625 -
Acta Biomater
Laminin alpha 4 promotes bone regeneration by facilitating cell adhesion and vascularization. [Abstract]2021 May:126:183-198. PMID: 33711525 -
Free Radic Biol Med
2024 Dec 9:227:296-311. PMID: 39653130 -
Mater Today Nano
Ligand Presentation Inside Protein Crystal Nanopores: Tunable Interfacial Adhesion Noncovalently Modulates Cell Attachment. [Abstract]2023 Dec:24:100432. PMID: 38370345 -
ACS Appl Mater Interfaces
Flower-like Mn-Doped Magnetic Nanoparticles Functionalized with αvβ3-Integrin-Ligand to Efficiently Induce Intracellular Heat after Alternating Magnetic Field Exposition, Triggering Glioma Cell Death. [Abstract]2019 Jul 31;11(30):26648-26663. PMID: 31287950 -
Cell Mol Gastroenterol Hepatol
MFAP4 Deficiency Attenuates Liver Fibrosis by Regulating Hepatic Stellate Cell Fate through Inhibition of the FAK/PI3K/NFκB Signaling Pathway. [Abstract]2025 May 29:101548. PMID: 40449846 -
Antioxidants (Basel)
An RGD-Conjugated Prodrug Nanoparticle with Blood-Brain-Barrier Penetrability for Neuroprotection Against Cerebral Ischemia-Reperfusion Injury. [Abstract]2024 Nov 1;13(11):1339. PMID: 39594481 -
Mol Ther Nucleic Acids
LOXL1 exerts oncogenesis and stimulates angiogenesis through the LOXL1-FBLN5/αvβ3 integrin/FAK-MAPK axis in ICC. [Abstract]2021 Jan 9;23:797-810. PMID: 33614230 -
Drug Deliv Transl Res
RGD-coated polymeric microbubbles promote ultrasound-mediated drug delivery in an inflamed endothelium-pericyte co-culture model of the blood-brain barrier. [Abstract]2024 Oct;14(10):2629-2641. PMID: 38498080 -
ACS Biomater Sci Eng
Regulation of Macrophage Polarization on Chiral Potential Distribution of CFO/P(VDF-TrFE) Films. [Abstract]2023 May 8;9(5):2524-2533. PMID: 37092816 -
Int Immunopharmacol
TAMs-derived SPP1, regulated by HIF-1α/STAT3 signaling pathway, influences colorectal cancer malignant progression by activation of EMT via integrin αvβ3. [Abstract]2025 May 26:159:114947. PMID: 40424660 -
Biochim Biophys Acta Mol Basis Dis
Triiodothyronine promotes the proliferation and chemoresistance of cholangiocarcinoma cells via HIF-1α/Glut1-stimulated glycolysis. [Abstract]2025 Mar 31;1871(5):167814. PMID: 40168755 -
Heliyon
Progesterone modulates cell growth via integrin αvβ3-dependent pathway in progesterone receptor-negative MDA-MB-231 cells. [Abstract]2024 Jul 2;10(13):e34006. PMID: 39071644 -
Mol Biol Rep
Fibrinopeptide a promotes the proliferation and migration of vascular smooth muscle cells by regulating the integrin αVβ3/PI3K/AKT signaling pathway. [Abstract]2025 Feb 5;52(1):205. PMID: 39907881 -
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Biochem Biophys Res Commun
2023 Sep 3:671:124-131. PMID: 37300942 -
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Solvent & Solubility
DMSO : 100 mg/mL (139.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 33.33 mg/mL (46.44 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 130 mg/mL (181.14 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Simecek J, et al. Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of (68)Ga-NOPO-c(RGDfK). Mol Pharm. 2014 May 5;11(5):1687-95. [Content Brief]
[2]. Lopez-Rodriguez V, et al. Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical. Nucl Med Biol. 2015 Feb;42(2):109-14. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 1.3934 mL | 6.9668 mL | 13.9336 mL | 34.8340 mL |
| 5 mM | 0.2787 mL | 1.3934 mL | 2.7867 mL | 6.9668 mL | |
| 10 mM | 0.1393 mL | 0.6967 mL | 1.3934 mL | 3.4834 mL | |
| 15 mM | 0.0929 mL | 0.4645 mL | 0.9289 mL | 2.3223 mL | |
| 20 mM | 0.0697 mL | 0.3483 mL | 0.6967 mL | 1.7417 mL | |
| 25 mM | 0.0557 mL | 0.2787 mL | 0.5573 mL | 1.3934 mL | |
| 30 mM | 0.0464 mL | 0.2322 mL | 0.4645 mL | 1.1611 mL | |
| 40 mM | 0.0348 mL | 0.1742 mL | 0.3483 mL | 0.8708 mL | |
| DMSO | 50 mM | 0.0279 mL | 0.1393 mL | 0.2787 mL | 0.6967 mL |
| 60 mM | 0.0232 mL | 0.1161 mL | 0.2322 mL | 0.5806 mL | |
| 80 mM | 0.0174 mL | 0.0871 mL | 0.1742 mL | 0.4354 mL | |
| 100 mM | 0.0139 mL | 0.0697 mL | 0.1393 mL | 0.3483 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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