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 dihydrochloride

CAS No. : 1431697-86-7

MCE 站：AT7867 dihydrochloride

产品活性：AT7867 dihydrochloride 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: 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

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 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域；
•   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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。