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PI 3-K/mTOR Inhibitor III, PKI-179
1-(4-(4-(3-Oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-morpholino-1,3,5-triazin-2-yl)-phenyl)-3-(pyridin-4-yl)urea, hydrate, N-(4-(4-(4-Morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl)phenyl)-N′-4-pyridinylurea, hydrate, PI 3-K Inhibitor XVII, mTOR Inhibitor X
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.
产品信息
Form White solid
Molar mass 506.6
Protect from Light 是的
Hygrocopic 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C25H28N8O3•H2O
CAS number 1197160-28-3
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Regulatory Review |