We report the following novel findings: (1) TKSE inhibited the proliferation of colorectal cancer cells by inhibiting the Akt/mTOR and ERK signaling pathways and activating AMPK, thus inducing apoptosis, (2) TKSE inhibited the metastatic abilities of colorectal cancer cells through the HIF-1α/VEGF pathway, and (3) TKSE exerted the anti-tumor effect without causing any observed toxic effects in our CT-26 tumor-bearing mouse model. Here, MTOR is linked to neoplasm.