CGP52411 是一种具有口服活性的 ATP 竞争性 EGFR 抑制剂（IC50：0.3 μM）。 CGP52411 阻止 Ca2+ 离子有毒流入神经元细胞，并显着抑制和逆转 β-淀粉样蛋白 Aβ42 原纤维聚集体的形成。 CGP52411 可用于阿尔茨海默病的研究。

CGP52411 is an orally active, and ATP-competitive inhibitor of EGFR (IC50: 0.3 μM). CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells and dramatically inhibits and reverses the formation of β-amyloid Aβ42 fibril aggregates. CGP52411 can be used in studies about Alzheimer's diseases.

In A431 cells, CGP52411 (0-100 μM) dose-dependently inhibits autophosphorylation and c-src autophosphorylation with IC50s of 1 μM and 16 μM, respectively. CGP52411 reduces tyrosine phosphorylation of p185c-erbB2 in a concentration-dependent manner(IC50 = 10 μM)[1]. CGP52411 inhibits c-src kinase (IC50 = 16 μM) and PKC isozymes isolated from porcine brain (IC50 = 80 μM)[1].

In female BALB/c nude mice, CGP52411 (6.3 mg/kg-50 mg/kg; orally) shows antitumor efficacy[1].

145915-58-8

C20H15N3O2

329.35

DAPH

DMSO:90mg/mL (273.3mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years