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A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC₅₀ = 0.42 nM) and PI 3-K (IC₅₀ = 8, 24, 74, 77, 14, and 11 nM against isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC₅₀ >50 µM), Cytochrome CYP isoforms, or hERG. It is reported to be orally available in mouse, rat, monkey, and dog species, and effectively suppress cancer growth both in cultures in vitro (IC₅₀ = 22 and 29 nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (by 30% of control MDA361 tumor size on day 42; 50 mg/kg/day p.o.) via apoptosis induction as a result of Akt/mTOR pathway inhibition.,官网链接:https://www.sigmaaldrich.cn/product/mm/526561
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