MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

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  |  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  |  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

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

货号: HY-12059

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。