iMDK quarterhydrate

iMDK quarterhydrate 是一种有效的 PI3K 抑制剂，可抑制生长因子 MDK（也称为中期因子或 MK）。iMDK quarterhydrate 与 MEK 抑制剂协同抑制非小细胞肺癌 (NSCLC)，而不会伤害正常细胞和小鼠。

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Background

iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice[1].

PD0325901 enhances growth inhibition in H441, H2009 and H520 and A549 NSCLC cells after iMDK quarterhydrate treatment[1].iMDK (50-500 nM) quarterhydrate suppressed AKT phosphorylation in a dose-dependent manner in H441 lung adenocarcinoma cells after treatment for 72 h. In contrast, iMDK quarterhydrate robustly increases p-ERK[1].

The combination treatment of iMDK ( (9 mg/kg/day; intraperitoneally injected with 100 μl) and PD0325901 (5 mg/kg; orally administered) effectively reduced lung tumor growth in a xenograft mouse model[1].

[1]. Naomasa Ishida, et al. A novel PI3K inhibitor iMDK suppresses non-small cell lung Cancer cooperatively with A MEK inhibitor. Exp Cell Res. 2015 Jul 15;335(2):197-206.