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AT7867

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 | Protein Tyrosine Kinase/RTK | 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 K_i 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 | Protein Tyrosine Kinase 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 | Staurosporine | H-89 dihydrochloride | Bucladesine sodium | Honokiol | 8-Bromo-cAMP sodium salt | Fasudil Hydrochloride | GSK-690693 | Artemisinin | PF-4708671 | Oridonin | Perifosine | Guggulsterone | Miransertib | Triciribine | Recilisib | SU6656 | Isobavachalcone | Scutellarin | K-252a | Deguelin | Miltefosine | A-674563 hydrochloride | Carnosol | Pluripotin | α-Linolenic acid | YS-49 | LJH685 | Urolithin B | Metadoxine

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