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CAS No. : 857531-00-1
MCE 国际站:AT7867
产品活性:AT7867 是一种 ATP 竞争性的 Akt1/Akt2/Akt3 和 p70S6K/PKA 抑制剂,IC50 分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM。
研究领域:PI3K/Akt/mTOR | Stem Cell/Wnt | MAPK/ERK Pathway
作用靶点:Akt | PKA | Ribosomal S6 Kinase (RSK)
In Vitro: The inhibition of AKT2 by AT7867 is shown to be ATP-competitive with a Ki of 18nM. AT7867 also displays potent activity against the structurally related AGC kinases p70S6K and PKA, but shows a clear window of selectivity against kinases from other kinase sub-families. In vitro growth inhibition studies show that AT7867 blocks proliferation in a number of human cancer cell lines. AT7867 appears to be most potent at inhibiting proliferation in MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines (IC50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC50 values range from 10-12 μM) .
In Vivo: In vivo: Following oral administration at 20 mg/kg, the elimination of AT7867 from plasma appears to be similar to that observed after i.v. administration. Plasma levels of AT7867 remain above 0.5 μM for at least 6 hours following an oral dose of 20 mg/kg. Assuming linear pharmacokinetics following i.v. administration, the bioavailability by the oral route is calculated to be 44%. In vivo pharmacodynamic (PD) biomarker studies are therefore performed with this model. Following pharmacokinetic and tolerability studies, doses of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) are administered to athymic mice bearing MES-SA tumors and the phosphorylation status of GSK3β and S6RP in tumors is monitored over time. Clear inhibition of phosphorylation of the two markers of pathway activity is seen at 2 and 6 hours following treatment with AT7867. By 24 hours, total levels of both GSK3β and S6RP are greatly reduced.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton 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 | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Staurosporine | LM22B-10 | SL 0101-1 | Insulin Detemir | (rac)-AG-205 | Rp-cAMPS | Cys-Kemptide | Multi-kinase-IN-2 | Akt/SKG Substrate Peptide | AS1949490 | RSK2-IN-3 | 1,3-Dicaffeoylquinic acid | Threo-Chloramphenicol-d6 | AKT-IN-14 | NSC45586 | APN/AKT-IN-1 | MS5033 | Sophocarpine monohydrate | MS143 | Deferoxamine | Chaetominine | Hu7691 free base | AKT-IN-3 | 8-Aminoadenosine | Nrf2/HO-1 activator 2 | AT13148 | CKI-7 free base | FMK-MEA
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