Allitinib 是可口服的EGFR和ErbB2不可逆抑制剂，IC50分别为 0.5 和 3 nM。它具有抗癌活性，抑制ErbB4，IC50为 0.8 nM。
产品描述
Allitinib (AST-1306) has anti-cancer activity，and it is an irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. [1]
体外活性
AST1306 (AST-1306; 0.19-6.25 μM; 72 hours) inhibit the growth of HIH3T3-EGFR T790M/L858R cells[1]. AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1]. AST1306 inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells，and dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells[1].
体内活性
AST1306 (AST-1306; oral; 25-100 mg/kg) significantly inhibited tumor growth in SK-OV-3 and Calu-3 xenograft models[1].
Cas No.
897383-62-9
分子式
C24H18ClFN4O2
分子量
448.88
别名
ALS 1306;AST-1306
储存和溶解度
DMSO:20mg/mL (44.56mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
