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Capivasertib
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Capivasertib
CAS No. : 1143532-39-1
MCE 站:Capivasertib
产品活性:Capivasertib (AZD5363) 是一种口服有效的 pan-AKT 激酶抑制剂,抑制 Akt1,Akt2 和 Akt3,IC50 分别为 3,7 和 7 nM。
研究领域:PI3K/Akt/mTOR | Autophagy
In Vitro: Capivasertib, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of 10 nM or less. Capivasertib inhibits phosphorylation of these substrates with an IC50 value of 0.06 to 0.76 μM in the 3 cell lines. Capivasertib 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, Capivasertib 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. AZD5363Capivasertibhibitor MK-2206 is much less active (IC50>30 μM).
In Vivo: Oral dosing of Capivasertib (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 Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Diabetes Related Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Honokiol | GSK-690693 | Artemisinin | Perifosine | Oridonin | Guggulsterone | Miransertib | SU6656 | Triciribine | Scutellarin | Isobavachalcone | Recilisib | Deguelin | A-674563 hydrochloride | Miltefosine | YS-49 | α-Linolenic acid | Urolithin B | Pachymic acid | 3CAI | Polyphyllin I | 1,3-Dicaffeoylquinic acid | Esculetin | Licochalcone E | Cyclovirobuxine D | GSK2110183 analog 1 hydrochloride | SC66 | Akt1 and Akt2-IN-1 | Arnicolide D
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热门标签:AZD5363