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CAS No. : 1047644-62-1
MCE 国际站:Afuresertib
产品活性:Afuresertib (GSK2110183) 是一个口服有效的,ATP 竞争性的选择性 pan-Akt 抑制剂,作用于 Akt1/Akt2/Akt3,Ki 值分别为 0.08/2/2.6 nM。
研究领域:PI3K/Akt/mTOR | TGF-beta/Smad | Epigenetics | Stem Cell/Wnt | Cytoskeleton | Cell Cycle/DNA Damage
作用靶点:Akt | PKC | ROCK
In Vitro: Afuresertib (GSK2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response.
In Vivo: Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing 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 | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Glucose Metabolism Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Rare Diseases Drug Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Coagulation and Anti-coagulation Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | SB-218078 | p32 Inhibitor M36 | Staurosporine | LM22B-10 | N-Myristoyl-Lys-Arg-Thr-Leu-Arg | PF-04577806 | Insulin Detemir | (rac)-AG-205 | Bisindolylmaleimide II | Hypericin | Multi-kinase-IN-2 | Akt/SKG Substrate Peptide | Chroman 1 dihydrochloride | D-erythro-Sphingosine | AS1949490 | 1,3-Dicaffeoylquinic acid | Mitoxantrone diacetate | Ripasudil free base | Threo-Chloramphenicol-d6 | AKT-IN-14 | NSC45586 | APN/AKT-IN-1 | R 59-022 hydrochloride | MS5033 | AS1892802 | Sophocarpine monohydrate | Ingenol Mebutate | MS143 | Deferoxamine | Chaetominine
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