Ganetespib (also known as STA-9090), 5-[2,4-dihydroxy-5-(1 methylethyl)phenyl]-2,4 dihydro-4-(1-methyl-1H indol-5 yl)-3H-1,2,4 triazole-3-one, is a potent small-molecule inhibitor of heat shock protein 90 (Hsp90), which binds to the ATP pocket in the N-terminus of Hsp90 resulting in down-regulation of Hsp90 client protein levels. Being structurally unrelated to geldanamycin-derived Hsp90 inhibitors (17-AAG, 17-DMAG, and IPI-504), ganetespib has a unique triazolone-containing chemical structure and stands out other Hsp90 inhibitors in terms of potency, antitumor activity, and safety profile. Results of previous studies indicate that ganetespib exhibits antitumor activity against a broad range of human cancers, including lung cancer, prostate cancer, colon cancer, breast cancer, melanoma and leukemia.
Reference
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