c-Met-IN-2

c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC₅₀ of 0.6 nM, with antitumor activity. IC50 & Target: IC50: 0.6 nM (c-Met)^[1] In Vitro: 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). In Vivo: 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].