纯度:99% by HPLC;NMR (Conforms)
分子式:C19H21F2N7O2
分子量:417.41
溶剂:DMSO (20 mg/ml) Ethanol (2.5 mg/ml)
性状:White or off-white solid
存储:-20°C
Activity (short version):PI 3-kinase inhibitor
Function / Pharmacology:Novel Class I phosphatidylinositol 3-kinase (PI3K) inhibitor. ZSTK474 is an ATP-competitive inhibitor of all four Class I PI3K isoforms. However, it inhibits PI3Kδ most potently, with a Ki of 1.8 nM, while inhibiting the α, β and γ isoforms at slightly higher concentrations (6.7 nM, 10.4 nM and 11.7 nM, respectively)1. Displays potent antitumor activity against human cancer xenografts (A549, PC-3 and WiDr) when administered to mice2. It displays potent anti-inflammatory activity via modulation of human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis3. Ameliorates the progression of adjuvant-induced arthritis in a rat model4.