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。

ETP-46321

CAS No. : 1252594-99-2

MCE 站：ETP-46321

产品活性：ETP-46321 是一种有效的 PI3Kα 和 PI3Kδ 抑制剂，K_iapp 分别为 2.3 和 14.2 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (K_iapp=2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (K_iapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC₅₀ of 8.3 nM.

In Vivo: ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor 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  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  3-Methyladenine  |  LY294002  |  Wortmannin  |  Quercetin  |  740 Y-P  |  PI-103  |  Isorhamnetin  |  Recilisib  |  Autophinib  |  AZD 6482  |  PI3K-IN-1  |  TG100-115  |  α-Linolenic acid  |  TGX-221  |  1-Deoxynojirimycin  |  YS-49  |  AS-605240  |  PKI-402  |  Disitertide  |  Erucic acid  |  CNX-1351  |  GSK1059615  |  Sonolisib  |  1,3-Dicaffeoylquinic acid  |  GNE-317  |  Esculetin  |  HS-173  |  Oroxin B

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。