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。

CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC 50 =27 nM) with apparent dissociation constants (K d ) of 19 nM.

Solid

PI3Kβ 1.1 μM (IC50) PI3Kδ 8.194 μM (IC

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). has not independently confirmed the accuracy of these methods. They are for reference only.

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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Bergamini G, et al. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012 Apr 29;8(6):576-82.

In Vitro: DMSO : ≥ 53 mg/mL (145.44 mM)配制储备液