EGFR Inhibitor 是一种 4,6-二取代的嘧啶,可诱导细胞凋亡,具有抗肿瘤活性。它是ATP竞争性,不可逆且高度选择性的EGFR抑制剂,IC50为 21 nM。它对EGFR的选择性高于 HER4 和 55种HERs" style="display: inline; color: #c13a36">其他激酶。它还抑制突变型EGFRL858R和EGFRL861Q,IC50分别为 63 nM 和 4 nM。
产品描述
EGFR inhibitor is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.
体外活性
EGFR Inhibitor possesses an enzymatic IC50= 21 nM against EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR Inhibitor also potently inhibits two EGFR mutants associated with clinical response to gefitinib: L858R (IC50: 63 nM) and L861Q (IC50: 4 nM), but displays much weaker activity against Her 4 (IC50: 7640 nM).
Cas No.
879127-07-8
分子式
C21H18F3N5O
分子量
413.404
别名
EGFR Inhibitor
储存和溶解度
Ethanol:10 mg/mL
DMSO:25 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years