Product name: Cilengitide
CAS NO.: 188968-51-6
Counter ion: Trifluoacetate
Format: Lyophilized powder
Description: Cilengitide (EMD121974; MSC1097999C) is a homodetic, head‐to‐tail cyclized Arg-Gly-Asp (RGD)‐containing pentapeptide with the chemical structure cyclo(Asp-d-Phe-N-MeVal-Arg-Gly). The physicochemical properties of the drug include molecular formula C27H40N8O7, molecular mass of 588.67 g/mol, partition coefficient Po/w of 0.0096 (log Po/w = −2.0), and hygroscopic. Cilengitide is a potent and selective antagonist of the αvβ3 and αvβ5 integrin receptors, that are involved in tumor cell growth and the formation of new tumor-related blood vessels (angiogenesis) in the tumor microenvironment and are overexpressed or aberrantly expressed in many cancers. By blocking integrins, tumor angiogenesis is prevented, providing the prospect of broader spectra of indications for cilengitide (e.g., glioblastoma, advanced solid tumors, pancreatic, prostate, nonsmall cell lung, and head and neck cancer). Experimental studies have shown that cilengitide demonstrates antiangiogenic, direct antitumor and antimigratory properties, and can suppress angiogenesis and tumor growth in vitro and in vivo. Cilengitide acts both as a monotherapy and as an enhancer of coadministered therapies, and affects cell proliferation of both tumor and vascular compartments.
Usage: For Scientific Research Use Only, Not for Human Use.