AMPC is a potent and effective TFF3 inhibitor. AMPC inhibits cell proliferation, survival, oncogenicity, and CSC-like behaviour in TFF3-positive CMS4 CRC cells. AMPC acts as a potential anti-cancer agent alone or in combination with 5-FU, and can be used for cancer research[1].
AMPC decreases cell proliferation in CMS4 CRC cells, the IC50 values are 2.63 μM, 4.65 μM, and 69.69 μM, respectively in SW620 (high TFF3 expression), Caco-2, SW480 cells (low TFF3 expression), respectively[1].AMPC (1-10 μM) significantly reduces the total cellular levels of TFF3 in SW620 and Caco2 cells in a dose dependent manner[1].AMPC induces apoptosis in a dose dependent manner by the inhibition of TFF3, it induces a decrease in the S-phase population and increases caspase3/7 activity compared with control cells[1].
AMPC (intraperitoneal injection; 40 mg/kg; once daily) leads to a significant reduction of tumour volume in AMPC-treated mice as compared to vehicle-treated mice from day 11 onward. AMPC results in larger areas of tumour necrosis and increased area of cells with apoptotic features in SW620 tumours. AMPC also significantly reduces tumour and serum TFF3 levels in vivo.
[1]. Ru-Mei Chen, et al. Pharmacological Inhibition of TFF3 Enhances Sensitivity of CMS4 Colorectal Carcinoma to 5-Fluorouracil through Inhibition of p44/42 MAPK. Int J Mol Sci. 2019 Dec 9;20(24):6215