AT13387 (trifluoroacetate)

AT13387 trifluoroacetate is a potent inhibitor of Hsp90, with K_d of 0.71 nM. IC50 & Target: Kd: 0.71 nM (Hsp90)^[1] In Vitro: AT13387 trifluoroacetate is a potent inhibitor of Hsp90, with K_d of 0.71 nM. AT13387 (Compound 35) shows potent antiproliferative activity in HCT116 cells, with an IC₅₀ of 31 nM. AT13387 also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC₅₀ of < 100 nM^[1]. AT13387 exhibits cytotoxic activity against many of the PPTP cell lines, with median IC₅₀ of 41 nM^[2]. In Vivo: AT13387 (60 mg/kg, ip 3 days on and 3 days off for four cycles) shows antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts^[1]. AT13387 (40 or 60 mg/kg, i.p.) induces significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts^[2].