CAS:936890-98-1
中文名：OSI-027
英文名：OSI-027
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OSI-027 的生物活性
OSI027 is a potent mammalian target of rapamycin (mTOR) kinase inhibitor. OSI027 has potential antineoplastic activity. MTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. MTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.
OSI027 acts as a potent suppressor of primitive leukemic precursors. OSI027 much more effective than rapamycin in eliciting antileukemic effects in vitro. OSI027 induces apoptosis of different types of cells transformed by the T315I-BCR-ABL mutation, which confers resistance to imatinib mesylate, nilotinib, and dasatinib. [1][2][3]
OSI-027 参考文献
[] Clin Cancer Res 2011;17:4378-4388
[] PNAS July 13, 2010;107:12469–12474
[] Autophagy October 1, 2010;6:7, 966-967
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