tcsc0969 Onalespib

Onalespib (AT13387) is a potent inhibitor of Hsp90, with a K_d of 0.71 nM.

IC50 & Target: Kd: 0.71 nM (Hsp90)^[1]

In Vitro: Onalespib (Compound 35) is a potent inhibitor of Hsp90, with K_d of 0.71 nM. Onalespib shows potent antiproliferative activity in HCT116 cells, with an IC₅₀ of 31 nM. Onalespib also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC₅₀ of < 100 nM^[1]. Onalespib exhibits cytotoxic activity against many of the PPTP cell lines, with median IC₅₀ of 41 nM^[2].

In Vivo: Onalespib (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]. Onalespib (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].