17-amino-17-demethoxygeldanamycin

IPI-493 is an orally bioavailable small molecule inhibitor of heat shock protein 90 (Hsp90), specifically formulated as the ansamycin derivative 17-amino-17-demethoxygeldanamycin (also known as 17-AG). It acts by binding to and inhibiting Hsp90, a molecular chaperone essential for the stability and function of multiple oncoproteins, including KIT, Akt, Bcr-Abl, EGFR, Flt3, c-Kit and PDGFRα. Inhibition of Hsp90 leads to degradation of these client proteins and results in growth inhibition or death in sensitive tumor cell populations. IPI-493 has demonstrated antitumor activity in preclinical models—particularly gastrointestinal stromal tumors (GIST) with heterogeneous KIT mutations—and has been evaluated in phase I clinical trials for advanced malignancies[1][4][5][6][7][8].

Other names

oral Hsp90 inhibitor IPI-493