AG-556

EGFR抑制剂(IC50=5µM)；对EGFR的选择性优于HER2(IC50=>500µM)；抑制EGF诱导的HER14细胞生长(IC50=3µM)；抑制过氧化氢诱导的表达TRPM2的HEK293细胞(IC50=0.94µM)以及3µM表达TRPA1的HEK293细胞中细胞内钙离子增加；以每天200µg/只动物的剂量降低EAE小鼠模型的发病率、严重程度和疾病持续时间；以10mg/kg的剂量减少脊髓组织中的水肿、脱髓鞘和MPO活性，并改善硬膜外压迫诱发的脊髓损伤小鼠模型的运动功能。An EGFR inhibitor (IC50 = 5 µM); selective for EGFR over HER2 (IC50 = >500 µM); inhibits EGF-induced growth of HER14 cells (IC50 = 3 µM); inhibits hydrogen peroxide-induced increases in intracellular calcium in HEK293 cells expressing TRPM2 (IC50 = 0.94 µM), as well as HEK293 cells expressing TRPA1 at 3 µM; reduces the incidence, severity, and duration of disease in a mouse model of EAE at 200 µg/animal per day; reduces edema, demyelination, and MPO activity in spinal cord tissue, as well as improves motor function in a mouse model of extradural compression-induced spinal cord injury at 10 mg/kg.分子式C20H20N2O3分子量336.4O=C(NCCCCC1=CC=CC=C1)/C(C#N)=C/C2=CC(O)=C(C=C2)O