AZD8055是一种高效选择性的、ATP竞争型的mTOR抑制剂,在MDA-MB-468细胞中IC50值为0.8 nM。AZD8055除了可以抑制mTORC1(p70S6K和4E-BP1)和mTORC2 (AKT) 以外,还完全抑制4E-BP1抗Rapamycin的T37/46磷酸化位点,明显地抑制cap-dependent转译作用,可有效地抑制U87MG, A549和H838等细胞增殖、诱导自体吞噬和导致LC3-II水平增加。在体外研究中,基于AZD8055作用于U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3和MES-SA移植瘤时,抑制pS6和pAKT,导致肿瘤生长受抑制,诱导肿瘤体积下降,表现出明显的抗癌活性。
参考文献
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冰袋运输。粉末直接保存于-20℃,有效期3年。易溶于DMSO。建议分装后-20℃避光保存,避免反复冻融。