SHetA2, a heterocyclic retinoid derivative, exhibits cytotoxic properties against cancer cells with an IC50 range of 0.37–4.6 μM. It promotes differentiation in cancer cells and induces cell apoptosis (apoptosis) via the mitochondrial intrinsic pathway, while arresting the cell cycle at the G2 phase. SHetA2 also demonstrates antitumor activity and favorable pharmacokinetic properties in mice, with oral activity.