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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(K_d^app) 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).

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