CZC24832

SKU: orb1226893

Description

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.

Key Properties

• CAS Number: 1159824-67-5
• MW: 364.4
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₇FN₆O₂S
• SMILES: O=S(C1=CC(C2=CN3C(C(F)=C2)=NC(N)=N3)=CN=C1)(NC(C)(C)C)=O
• Target: PI3K
• Solubility: DMSO: 5 mg/mL warmed (13.72 mM)

Bioactivity

• 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).
• 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CZC24832 | CZC-24832 | CZC 24832

Quick Database Links

Gene Symbol

PI3K