ETP 45658 是一种有效的 PI3K 抑制剂，对 PI3Kα、PI3Kδ、PI3Kβ 和 PI3Kγ 的 IC50 分别为 22.0 nM、39.8 nM、129.0 nM 和 717.3 nM。 ETP 45658 还可以抑制 DNA-PK (IC50\u003d70.6 nM) 和 mTOR (IC50\u003d152.0 nM)。 ETP 45658 可用于癌症研究。
PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively). Inhibits proliferation of multiple cancer cell lines in vitro and reduces Akt phosphorylation levels in vivo.
Link et al (2009) Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J.Biol.Chem. 284 28392 PMID:19690175 |Hill et al (2014) A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes. Breast Cancer Res. 16 482 PMID:25488803
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