PP242

mTORC1和mTORC2中mTOR激酶活性位点的抑制剂(IC50=8nM)；研究显示其比雷帕霉素更有效地导致白血病细胞死亡，并且在体内延迟白血病发作，并增强酪氨酸激酶抑制剂在抑制白血病扩散和延长生存期方面的作用。An inhibitor of the active site of mTOR kinase in both mTORC1 and mTORC2 (IC50 = 8 nM); shown to cause the death of leukemia cells more potently than rapamycin and, in vivo, delays leukemia onset and augments the effects of tyrosine kinase inhibitors in suppressing leukemic expansion and extending survival.