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αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine hydrochloride, (1S)-1-Benzyl-2-(5-(3-methyl-1H-indazol-5-yl)-pyridin-3-yloxy)-ethylamine hydrochloride, (2S)-1-(5-(3-methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine hydrochloride, A 674563 hydrochloride, A674563 hydrochloride
C22H22N4O · xHCl
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生化/生理作用
A-674563 is an orally available ATP-competitive pan-AKT (PKB, protein Kinase B) inhibitor (AKT1 Ki = 11 nM) with additional potency against PKA, Cdk2 GSK3β (IC50 = 1.4, 4.2,10 nM, respectively). A-674563 reduces the phosphorylation of cellular Akt substrates (0.1-10 μM; MiaPaCa-2) and enhances paclitaxel efficacy in a PC-3 xenograft model in mice in vivo (40 mg A-674563/kg via p.o. b.i.d. for 21 days, 15 mg paclitaxel/day on days 20, 24, 28).
WGK
WGK 3
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