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. 2013 Nov 25;110(50):20224–20229. doi: 10.1073/pnas.1314239110

Fig. 2.

Fig. 2.

LGK974 inhibits Wnt signaling in vivo and induces tumor regression in a mechanistic MMTV-Wnt1 tumor model. (A) LGK974 showed a strong efficacy in a Wnt tumor model (MMTV-Wnt) in nude mice. Spontaneous tumors from the MMTV-Wnt1 transgenic mice were implanted in nude mice. LGK974 was dosed at 0.3, 1.0, and 3.0 mg/kg per day for 13 d. LGK974 induced robust tumor regression at 1.0- and 3.0-mg/kg doses. (B) A PD study was performed in the murine MMTV-Wnt tumor model. LGK974 significantly inhibited AXIN2 expression 7 h after the last dose, and the effect diminished 24 h after the dose. (C) In the same PD study, pLRP6 expression level showed a very similar pattern to the PD response of AXIN2. LGK974 inhibitory effect peaked at 7 h after the last dose and diminished 24 h after the last dose.