Olmutinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Olmutinib 是一种新型表皮生长因子受体酪氨酸激酶抑制剂。Olmutinib 3 μM 通过拮抗 ABCG2 过表达细胞中的药物流出功能，显着逆转 ABCG2 介导的耐药性，但不能逆转 ABCB1 和 ABCC1 介导的耐药性。

Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib 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.

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BI1482694,HM61713

Angiogenesis

EGFR

EGFR

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1802181-20-9

486.6

C26H26N6O2S?

>98% (HPLC)

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CN1CCN(CC1)c1ccc(cc1)Nc1nc2c(c(n1)Oc1cccc(c1)NC(=O)C=C)scc2

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(-20℃)

With Ice Pack

≥ 2 years