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CZC24832
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CZC24832
CAS No. : 1159824-67-5
MCE 站:CZC24832
产品活性:CZC24832 是一种有效的选择性 PI3Kγ 抑制剂,IC50 为 27 nM,表观解离常数(Kdapp) 为 19 nM。
研究领域:PI3K/Akt/mTOR
作用靶点:PI3K
In Vitro: CZC24832 is active in PI3Kγ-dependent cellular C5a-induced AKT Ser473 phosphorylation (IC50=1.2 μM) and N-formyl-methionine-leucinephenylalanine (fMLP)-induced neutrophil migration assays (IC50=1.0 μM).
In Vivo: CZC24832 shows suitable pharmacokinetic properties including low clearance (0.84 L per h per kg body weight) and high oral bioavailability (37%), thus allowing further characterization of the inhibitor in rodent models of inflammation. In an IL-8-dependent air pouch model, CZC24832 shows a dose-dependent reduction of granulocyte recruitment (80% inhibition at 10 mg per kg body weight) consistent with the degree of inhibition observed in PI3Kγ-null mice. Mice treated orally with 10 mg CZC24832 per kg body weight twice per day show a substantial decrease of bone and cartilage destruction (53% reduction by histopathological analysis) as well as of overall clinical parameters (38% reduction).
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | 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 | 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
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