AS-041164 是选择性的,具有口服活性的PI3Kγ亚型抑制剂,IC50=70 nM。它对 PI3Kα (IC50:240 μM),PI3Kβ (IC50:1.45 μM) 和 PI3Kδ (IC50:1.70 μM) 的活性较低。它具有抗炎活性。
产品描述
AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects.
体内活性
AS-041164 (3-100 mg/kg p.o.) treatment dose-dependently decreases r-h regulated on activation normal T cell expressed and secreted (RANTES)-induced neutrophil recruitment in mice.?The ED50 value for AS-041164 is 27.35 mg/kg.?AS-041164 blocks RANTES-induced chemotaxis and reduces the level of AKT phosphorylation.?AS-041164 (10-100 mg/kg; oral administration; once) treatment results in the reduction of inflammatory swelling in the model of carrageenan-induced paw edema.
Cas No.
6318-41-8
分子式
C11H7NO4S
分子量
249.24
储存和溶解度
DMSO:125 mg/mL (501.52 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years