Description
An inhibitor of Hsp90 (IC50 = 0.14 µM); inhibits proliferation of a variety of cancer cell lines, including colon, prostate, ovarian, gastric, and breast cancer cells (IC50s = 0.2-0.55 µM), as well as MV4-11 leukemia, A549 NSCLC, NCI H69 SCLC, and multidrug-resistant NCI/ADR-RES cells (IC50s = 0.25, 0.77, 0.15, and 4.3 µM, respectively); induces degradation of Akt and HER2 (IC50s = 0.1-0.5 µM) and a compensatory Hsp70 response in NCI N87, HCT116, and DU145 cell lysates; induces Hsp70 expression in the liver and tumor tissue and reduces tumor growth in an NCI N87 mouse xenograft model at 50 and 75 mg/kg and tumor regression at 125 and 200 mg/kg