Anticancer agent 300

Anticanceragent 300 (compound P14) is a regulator of CCND1, CDK4, CDK6, and CCNE1, exhibiting antiproliferative, cell cycle regulatory, senescence-inducing, and apoptosis-inducing activities. Anticanceragent 300 is applicable in research on ER+/HER2− breast cancer and BRAF-mutant melanoma.

Anticancer agent 300 (P14) effectively reduces colony formation in MCF7 and A375 cells at concentrations of 5-50 μM over 7 days, with noted cytotoxicity at higher concentrations in non-tumorigenic TC28a2 cells. It exhibits IC50 values of 2.018 μM in MCF7 cells and 1.887 μM in A375 cells. Using 5 μM for 12 days, it significantly decreases spheroid size in 3D cultures of MCF7 and A375 cells. At 5 μM over 7 days, it reduces the proportion of G2/M phase cells in MCF7 and A375 lines and modulates cell cycle-related gene expression in a cell-specific manner, increasing G1/S transition genes in MCF7 cells and decreasing them in A375. It also elevates senescence-related gene expression in both cell types and differentially regulates SASP factors, increasing them in MCF7 and reducing in A375 cells. Additionally, it induces higher levels of cell death and promotes early apoptosis in MCF7 and A375 cells.