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。

Eganelisib

CAS No. : 1693758-51-8

MCE 站：Eganelisib

产品活性：Eganelisib (IPI549) 是一种有效的选择性 PI3Kγ 抑制剂，IC₅₀ 为 16 nM，选择性比其他脂类和蛋白质激酶高出 100 多倍。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: Eganelisib (IPI549) inhibits PI3Kγ with IC₅₀ of 16 nM, with >100-fold selectivity over other lipid and protein kinases (PI3Kα IC₅₀=3.2 μM, PI3Kβ IC₅₀=3.5 μM, PI3Kδ IC₅₀>8.4 μM). Eganelisib is evaluated for activity across all Class I PI3K isoforms. The binding affinity of Eganelisib for PI3K-γ is determined by measuring the individual rates constants and for PI3K-α, β and δ using equilibrium fluorescent titration. Eganelisib is a remarkably tight binder to PI3Kγ with a K_d of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα K_d=17 nM, PI3Kβ K_d=82 nM, PI3Kδ K_d=23 M). In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, Eganelisib demonstrates excellent PI3K-γ potency (IC₅₀=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Cellular IC₅₀s for Class I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) are determined in SKOV-3, 786-O, RAW 264.7, and RAJI cells, respectively, by monitoring inhibition of pAKT S473 by ELISA. Furthermore, Eganelisib dose dependently inhibits PI3Kγ dependent bone marrow-derived macrophage (BMDM) migration. Eganelisib is selective against a panel of 80 GPCRs, ion channels, and transporters at 10 μM.

In Vivo: Eganelisib (IPI549) demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration. In vivo (mice, rats, dog, and monkeys), Eganelisib has excellent oral bioavailability, low clearance, and distributed into tissues with a mean volume of distribution of 1.2 L/kg. Overall, Eganelisib has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. The t_1/2 of IPI-549 for mouse, rat, dog and monkey is 3.2, 4.4, 6.7 and 4.3 h, respectively. Eganelisib significantly reduces neutrophil migration in a dose dependent manner in this model when administered orally at all of the tested doses.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Oxygen Sensing Compound Library  |  Anti-COVID-19 Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton 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。