AG-1478 是一种选择性EGFR酪氨酸激酶抑制剂，IC50为 3 nM。它对HCV和脑心肌炎病毒有抗病毒作用。

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.

0.4 mg AG-1478与单剂量25 μCi 90Y-CHX-A''-DTPA-hu3S193联用,与单独药物相比,具有显著增强的效力.AG-1478给药阻断肿瘤位点的EGFR磷酸化,并抑制过表达wt EGFR 的A431异种移植物和表达de2-7 EGFR的胶质瘤异种移植物的生长.甚至亚治疗剂量的AG-1478也显著增强细胞毒性药物的效力,AG-1478和替莫唑胺联用对人类神经胶质瘤异种移植物显示出协同的抗肿瘤活性.

0.25 μM AG-1478在VSMC 中,消除Ang II,Ca2+离子载体以及EGF诱导的MAPK活化,但是不影响佛波酯或血小板源生长因子-BB诱导的MAPK活化。AG-1478抑制EGF诱导的BaF/ERX和LIM1215细胞有丝分裂,IC50分别为0.07 μM和0.2 μM。AAG1478能够抑制ABC结合盒（ABC）转运蛋白（如ABCB1和ABCG2）的功能,对ABCG2有更显著的影响。与表达内源性wt EGFR或过表达外源性wt EGFR的细胞相比（IC50分别为34.6 μM和48.4 μM）,AG-1478优先抑制表达ΔEGFR的U87 mg细胞,IC50为8.7 μM。与内源性或过表达的外源性wt EGFR 相比,AG-1478也会优先抑制酪氨酸激酶活性和ΔEGFR的自磷酸化。

Cells are exposed to different concentrations of AG-1478 for 72 hours in 96-well plates. The effects of AG-1478 on cell growth are examined using an Alamar Blue assay. A 20-μL aliquot of Alamar Blue is added to each well, and its absorbance is determined using a Spectromax Scanning Micro plate Reader. The effects of AG-1478 are expressed as percentage of growth inhibition using untreated cells as the control (0% inhibition). Cellular DNA synthesis is determined using a [3H]thymidine incorporation assay. (Only for Reference)

153436-53-4

C16H14ClN3O2

315.76

AG1478;Tyrphostin AG-1478;NSC 693255

Ethanol:11 mg/mL (34.8 mM)
DMSO:24 mg/mL (76 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years