AZD8931 diFuMaric acid 是一种可逆的 ATP 竞争性 EGFR、ErbB2 和 ErbB3 抑制剂(IC50 分别为 4 nM、3 nM 和 4 nM)。
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AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively).
体内活性
AZD8931 significantly suppressed cell growth of IBC cells and induced apoptosis of human IBC cells in vitro.AZD8931 monotherapy inhibited xenograft growth[1].
动物实验
Two IBC cell lines SUM149 and FC-IBC-02 。Cell growth and apoptotic cell death were examined in vitro.?For the in vivo tumor growth studies, IBC cells were orthotopically transplanted into the mammary fat pads of immunodeficient mice.?AZD8931 was given by daily oral gavage at doses of 25 mg/kg, 5 days/week for 4 weeks.?Paclitaxel was subcutaneously injected twice weekly[1].
Cas No.
1196531-39-1
分子式
C31H33ClFN5O11
分子量
706.08
别名
4-[[4-[(3-氯-2-氟苯基)氨基]-7-甲氧基-6-喹唑啉基]氧基]-N-甲基-1-哌啶乙酰胺二富马酸盐;AZD8931 diFuMaric acid
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years