产品描述:
Tegatrabetan is an inhibitor of Wnt/β-catenin signaling.{67484} It reduces Wnt3a-induced transcriptional activity in a reporter activity assay using STF3a cells, which exhibit constitutive Wnt activation, when used at a concentration of 1 µM. Tegatrabetan inhibits proliferation of, and transcription in, HT-29 human colon cancer cells (IC50s = 9 and 63 nM, respectively) and reduces survival in six other cancer cell lines (IC50s = 14-80 nM). It induces cell cycle arrest at the G1 phase in HCT-15 human colon cancer cells when used at a concentration of 625 nM. In vivo, tegatrabetan (50 mg/kg per day) reduces tumor volume and inhibits lung metastasis in a Saos-2 osteosarcoma mouse xenograft model.{67485}