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Cyclo (-RGDfK) (TFA)

Cyclo (-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM[1]. Cyclo (-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[3].

Product Specifications

CAS Number

[500577-51-5]

UNSPSC

12352209

Hazard Statement

H302, H315, H319, H335

Target

Integrin

Type

Peptides

Related Pathways

Cytoskeleton

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cyclo-rgdfk-tfa.html

Purity

99.82

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 33.33 mg/mL (ultrasonic)

Smiles

O=C(O)C(F)(F)F.O=C([C@H](CCCCN)NC([C@@H](CC1=CC=CC=C1)NC([C@H](CC(O)=O)NC(CN2)=O)=O)=O)N[C@@H](CCCNC(N)=N)C2=O

Molecular Formula

C29H42F3N9O9

Molecular Weight

717.69

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture)

Scientific Category

Peptides

Clinical Information

No Development Reported

Isoform

αvβ3

Citation 01

ACS Biomater Sci Eng. 2023 May 8;9 (5) :2524-2533.|Cell Mol Gastroenterol Hepatol. 2025 May 29:101548.|Int Immunopharmacol. 2025 May 26:159:114947.|ACS Appl Mater Interfaces. 2019 Jul 31;11 (30) :26648-26663. |Acta Biomater. 2021 May:126:183-198.|Adv Healthc Mater. 2021 Jul;10 (13) :e2100304.|Adv Sci (Weinh) . 2025 Oct 30:e01602.|Antioxidants (Basel) . 2024 Nov 1;13 (11) :1339.|Bioact Mater. 2021 Jan 7;6 (7) :2039-2057.|Biochem Biophys Res Commun. 2023 Sep 3:671:124-131.|Biochim Biophys Acta Mol Basis Dis. 2025 Mar 31;1871 (5) :167814.|bioRxiv. 2024 July 13.|bioRxiv. 2025 April 01.|Bone Res. 2024 Aug 28;12 (1) :49.|Drug Deliv Transl Res. 2024 Oct;14 (10) :2629-2641.|Engineering. 8 October 2020.|Free Radic Biol Med. 2024 Dec 9:227:296-311.|Heliyon. 2024 Jul 2;10 (13) :e34006.|J Extracell Vesicles. 2025 Aug;14 (8) :e70146.|J Nanobiotechnology. 2024 Sep 1;22 (1) :528.|Mater Today Nano. 2023 Dec:24:100432.|Mol Biol Rep. 2025 Feb 5;52 (1) :205.|Mol Ther Nucleic Acids. 2021 Jan 9;23:797-810.|Res Sq. 2024 Aug 07.

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