TAS-116

TAS-116 是有效的且有选择性的 HSP90α/β 抑制剂,Ki 值分别为 34.7 nM,21.3 nM。

研究领域 >> 癌症

HSP90α:34.7 nM (Ki)

HSP90β:21.3 nM (Ki)

[1]. Kitade, Makoto; Ohkubo, Shuichi; Yoshimura, Chihoko; et al. Preparation of azabicyclo compounds and salts thereof as inhibitors of heat-shock proteins HSP 90. PCT Int. Appl. (2011), WO 2011004610 A1 20110113.

[2]. Ohkubo S, et al.TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther. 2015 Jan; 14(1):14-22.

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