CZC24832

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CZC24832 是 PI 3-kinase γ 的选择性抑制剂（在 PI 3-Kγ 依赖性 fMLP 诱导的中性粒细胞迁移测定中，IC50 = 1.0 μM）。

CZC24832 is a selective inhibitor of PI 3-kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay); exhibits limited off-target effects in kinome profiling of 154 identified lipid and protein kinases and 922 other proteins.

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).

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).

CZC24832 | CZC-24832 | CZC 24832

PI3K/Akt/mTOR signaling

PI3K

PI3Kβ| PI3Kγ| PI3Kδ

Inflammation/Immunology

——

1159824-67-5

364.4

C15H17FN6O2S

>98% (HPLC)

DMSO: 5 mg/mL warmed (13.72 mM)

O=S(C1=CC(C2=CN3C(C(F)=C2)=NC(N)=N3)=CN=C1)(NC(C)(C)C)=O

5-(2-amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)pyridine-3-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years