cilengitide-tfa

Description: Cilengitide TFA (also known as EMD 121974, NSC 707544), the trifluoroacetic acid salt of cilengitide, is a highly potent and selective integrin inhibitor for the alphavbeta3 receptor and the alphavbeta5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; it showed ca.10-fold selectivity against gpIIbIIIa. Cilengitide is a cyclic Arg-Gly-Asp based peptide with potential antineoplastic activity and has been extensively studied for its anticancer application. The mechanism of action for cilengitide is to bind to and inhibit the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. Cilengitide is currently undergoing phase 2 clinical trials, and the European Medicines Agency has granted cilengitide orphan drug status.

References: Cancers (Basel). 2017; 9(9): 117; Genes Cancer. 2011 Dec; 2(12):1159-65; Cancer Res. 2002 Aug 1; 62(15):4263-72.

Related CAS#: 188968-51-6 (free base); 199807-35-7 (TFA)