Olmutinib 是一种新型表皮生长因子受体酪氨酸激酶抑制剂。

Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor

Olmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.?In addition, olmutinib at reversal concentration affected neither the protein expression level nor the localization of ABCG2.?The results observed from the accumulation/efflux study of olmutinib showed that olmutinib reversed ABCG2-mediated MDR with an increasing intracellular drug accumulation due to inhibited drug efflux.?We also had consistent results with the ATPase assay that olmutinib stimulated ATPase activity of ABCG2 up to 3.5-fold.?Additionally, the molecular interaction between olmutinib and ABCG2 was identified by docking simulation.?Olmutinib not only interacts directly with ABCG2 but also works as a competitive inhibitor of the transport protein[1]

1802181-20-9

C26H26N6O2S

486.6

HM61713;BI1482694;Olmutinib

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years