产品描述:
TAS 116 is a heat shock protein 90 (Hsp90) inhibitor.{58495} 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.