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Since Hsp90 plays an important role in the conformational maturation, stability and function of some oncogenic proteins, the inhibitors of Hsp90 are developed as therapeutic for cancers. NMS-E973 is a selective inhibitor of Hsp90. It binds to Hsp90α within the ATP binding site with DC50 value of < 10nM. Besides that, NMS-E973 shows no effect on a panel of 52 various protein kinases such as ABL, ACK1, AKT1 and Alk. The IC50 value of it for Hsc70 is > 10μM. NMS-E973 exerts antiproliferation effects on A2780 tumor cell line and BT-474 breast cancer cell line with IC50 values of 69nM and 110nM, respectively. When treated with mice bearing A2780 xenografts, the intravenous administration of NMS-E973 significantly inhibits tumor growth with TGI value of 53% at dose of 30mg/kg. Moreover, NMS-E973 also displays antitumor activity in tumors resistant to kinase inhibitors such as vemurafenib [1, 2].

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