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c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.

c-Met-IN-2 (Compound 14) is a potent and selective c-Met inhibitor, with an IC50 of 0.6 nM. c-Met-IN-2 also shows weak activity on other kinases, with IC50s of 1075 nM (AxI), 731 nM (RON), 18364 nM (VEGFR2), 5396 nM (c-Kit), 2357 nM (PDGFRa), 17056 nM (c-Src).

c-Met-IN-2 (0.1, 1, 10 mg/kg, p.o., once daily) significantly reduces the volume of tumor in mice bearing H1993 tumors, and has similar effect in SNU-5 xenograft model via oral administration at 0.3, 1 and 3 mg/kg[1].

[1]. Zhao F, et al. Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization. Eur J Med Chem. 2017 Jul 7;134:147-158.

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