Cyclo(-RGDfK) TFA

Cyclo(-RGDfK) TFA (CAS No.: 500577-51-5) is a cyclic peptide trifluoroacetate salt based on the Arg-Gly-Asp (RGD) recognition sequence. As a selective antagonistic ligand of integrin αvβ3, a receptor enriched on angiogenesis-associated endothelial cells and various tumor cells, it is widely used in research fields such as tumor biology, vascular biology, and targeted delivery; derived from the RGD motif in extracellular matrix proteins, it specifically binds to cell-surface αvβ3 receptors and competitively blocks their interaction with endogenous RGD-containing ligands, thereby modulating adhesion-dependent signaling cascades in vitro, including focal adhesion kinase/Src, PI3K–Akt, and MAPK pathways, and consequently affecting cell adhesion, migration, and related phenotypes. Reported in vitro activity indicates high-affinity inhibition of αvβ3-mediated ligand binding in the single-digit nanomolar range, consistent with the characteristics of a potent antagonist. As a trifluoroacetate salt form, the TFA counterion helps improve peptide stability and experimental biocompatibility, facilitating dissolution, preparation, and handling in the laboratory. Typical applications include cell adhesion/migration assays, receptor binding and competition assays, phenotypic and target-directed screening, and the development of conjugates or probes in cell and animal models for detecting αvβ3-positive tumor microvasculature and cancer cells; the concentration or dose used in experiments usually depends on the specific experimental design and research purpose. This product is for laboratory research use only and must not be used for human or veterinary purposes or in any clinical setting.