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HSP90??/HSP90?? inhibitor
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
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HSP90 抑制剂
CUDC-305 (DEBIO-0932) 是一种新型的热休克蛋白90(HSP90)抑制剂,对HSP90 alpha/beta具有很强的亲和力,对HSP90α和HSP90β的IC50值分别为100和103nM。具有很高的口服生物利用度,并且对多种癌细胞系均具有强大的抗增殖活性(平均IC50为220 nmol/L)。包括许多对护理标准(SOC)药物有抵抗力的非小细胞肺癌(NSCLC)细胞系。
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- Aykut Ozgur, .et al. Debio-0932, a second generation oral Hsp90 inhibitor, induces apoptosis in MCF-7 and MDA-MB-231 cell lines, Mol Biol Rep, 2021, Apr;48(4):3439-3449 PMID: 33999319