An Hsp90 inhibitor
TAS 116 is a heat shock protein 90 (Hsp90) inhibitor.1 It selectively binds to Hsp90α and Hsp90β (Kis = 34.7 and 21.3 nM, respectively) over glucose-regulated protein 94 (GRP94) and TGF-β receptor-associated protein 1 (TRAP1; Kis = 50,000 nM for both). TAS 116 (3.6, 7.1, and 14 mg/kg) reduces intratumoral protein levels of HER2, HER3, and Akt, as well as reduces tumor growth in a HER2-expressing NCI N87 gastric cancer mouse xenograft model and does not induce photoreceptor injury in rats when administered at a dose of 12 mg/kg per day.
1.Ohkubo, S., Kodama, Y., Muraoka, H., 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 modelsMol. Cancer Ther.14(1)14-22(2015)
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