AZD5363 1143532-39-1

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AZD5363 is a potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,2 and 3, respectively. IC50 & Target: IC50: 3 nM (Akt1), 7 nM (Akt2), 7 nM (Akt3), 6 nM (p70S6K), 7 nM (PKA), 60 nM (ROCK2) In Vitro: AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of 10 nM or less and inhibits phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μM. AZD5363 inhibits phosphorylation of these substrates with an IC50 value of 0.06 to 0.76 μM in the 3 cell lines. AZD5363 effectively inhibits phosphorylation of S6 and 4E-BP1 in these cell lines, whereas it increases phosphorylation of AKT at both ser473 and thr308. In BT474c cells, AZD5363 induces FOXO3a nuclear translocation with EC50 value of 0.69 μM; a concentration of 3 μM is sufficient to almost completely localize FOXO3a to the nucleus. AZD5363 inhibits S6 phosphorylation with an IC50 value of approximately 4.8 μM, whereas the allosteric inhibitor MK-2206 is much less active (IC50>30 μM)In Vivo: Oral dosing of AZD5363 to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50 ~ 0.1 μM total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of AZD5363 caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhances the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts.

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