Pt(IV)-biSi-2

Pt(IV)-biSi-2 is a novel platinum(IV) prodrug complex where both axial positions are occupied by bis-organosilane ligands, specifically synthesized as cis-dichloro(diisopropylamine)-trans-[3-(triethoxysilyl)propylcarbamate]platinum(IV). It demonstrates **enhanced cytotoxicity and selectivity against human colorectal cancer cells** (notably HCT 116 and HT-29) compared to cisplatin, while maintaining significantly reduced toxicity toward nontumorigenic intestinal cells (HIEC6)[1][2][3][4][5]. In preclinical mouse models of colorectal cancer, Pt(IV)-biSi-2 reduced tumor growth more effectively and at lower concentrations than cisplatin, with fewer side effects such as renal and hepatic toxicity. Mechanistically, Pt(IV)-biSi-2 acts as a prodrug that is rapidly reduced in the tumor microenvironment to active Pt(II) species, whereupon it induces **permanent, p53-independent DNA double-strand breaks**, in contrast to cisplatin's transient effects[1][2][3][4]. Cellular uptake of Pt(IV)-biSi-2 is superior to that of cisplatin, and its activity profile enables chronic dosing with better tolerability.

Other names

cis-dichloro(diisopropylamine)-trans-[3-(triethoxysilyl)propylcarbamate]platinum(IV)