[Description]
PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer[1]. PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively[1].
PI3K/mTOR Inhibitor-4 (2.5-10 µM; 24 h) inhibits the PI3K/AKT/mTOR pathway[1]. Cell Viability Assay[1] Western Blot Analysis[1] PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague-Dawley rats[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity[1]. |