6318-41-8

The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism. AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC₅₀ = 70 nM), compared to PI3Kα (IC₅₀ = 240 nM), PI3Kβ (IC₅₀ = 1.45 μM), and PI3Kδ (IC₅₀ =1.70 μM). When tested at 1.0 μM, it shows little or no activity against 38 other common kinases. When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED₅₀ = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.

AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects[1].

PI3Kγ: 70 nM (IC₅₀); PI3Kα: 240 nM (IC₅₀); PI3Kβ: 1.4 μM (IC₅₀); PI3Kδ: 1.7 μM (IC₅₀)

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1) Ferrandi et al. (2007) Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment: J. Pharmacol. Exp. Ther. 322 923