GM-60186 is a 5-HT receptor 2B (HTR2B) inhibitor with an IC50 of 257 nM. GM-60186 significantly inhibits colorectal cancer proliferation and migration [1].
In Vivo, GM-60186 (10-20 mg/kg; IP; daily; for 20 days) significantly reduces tumor size and weight in xenograft mouse models[1].
In Vitro, GM-60186 (50-500 nM; 72 hours) effectively inhibits the proliferation in colorectal cancer (CRC) cells[1]. GM-60186 (500 nM; 24-48 hours) effectively inhibits colorectal cancer migration[1].
References:
[1]. Jeong-Yun Lee, et al. Inhibition of HTR2B-mediated serotonin signaling in colorectal cancer suppresses tumor growth through ERK signaling. Biomed Pharmacother. 2024 Oct:179:117428.
In Vivo, GM-60186 (10-20 mg/kg; IP; daily; for 20 days) significantly reduces tumor size and weight in xenograft mouse models[1].
In Vitro, GM-60186 (50-500 nM; 72 hours) effectively inhibits the proliferation in colorectal cancer (CRC) cells[1]. GM-60186 (500 nM; 24-48 hours) effectively inhibits colorectal cancer migration[1].
References:
[1]. Jeong-Yun Lee, et al. Inhibition of HTR2B-mediated serotonin signaling in colorectal cancer suppresses tumor growth through ERK signaling. Biomed Pharmacother. 2024 Oct:179:117428.