Product Overview
Retaspimycin hydrochloride (also known as IPI-504), a hydroquinone hydrochloride salt derivative of 17-AAG, is a novel, potent and selective inhibitor of heat shock protein 90 (Hsp90) that binds to the amino-terminal ATP/ADP-binding site of Hsp90. As a highly water-soluble version of 17-AAG, IPI-504 (solubility >200 mg/mL) does not need prior dissolution in organic solvents and hence can be delivered in high concentrations. Once in the systemic circulation, IPI-504 is deprotonated and converted into the free base IPI-504 which is subsequently oxidized to 17-AAG. IPI-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration IC50 values ranging from 10-40 nmol/L and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer.
Chemical Name
[(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6,20,22-trihydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16-oxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(22),8,12,14,18,20-hexaen-10-yl] carbamate; hydrochloride