现货，GSK690693，selleck，美国进口，AKT 抑制剂

GSK690693 is an aminofurazan-derived，novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2, 13, and 9 nM respectively)versus the majority of kinases in other families; however, it does inhibit additional members of the AGC kinase family. ^[1,2]

GSK690693 inhibited proliferation and induced apoptosis in a subset of tumor cells with potency consistent with intracellular inhibition of Akt kinase activity. ^[1]

Daily administration of GSK690693 produced significant antitumor activity in mice bearing established human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts. ^[1]

• Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity Dirk A. Heerding, Derek R. Duckett, et al. Cancer Res 2008;68:2366-2374
• Identi?cation of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase Dirk A. Heerding,Nelson Rhodes,et al. J. Med. Chem 2008;51: 5663–5679

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