In vivo, SR9243 effectively curtails glycolysis and lipogenesis in tumors and triggers apoptosis in cancer cells, without causing weight loss. It restrains tumor proliferation and lipogenesis efficiently, avoiding liver toxicity or inflammation.

SR9243 targets LXR specifically, causing a dose-dependent decrease in LXR-mediated gene expression, effectively reducing LXRα- and LXRβ-driven transcription at nanomolar levels, and strongly inhibiting luciferase activity linked to LXR in cancer cell cultures. It significantly lowers the viability of cancer cells at nanomolar doses (IC50 approximately 15-104 nM) in lines from prostate (PC3 and DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancers. SR9243 also markedly diminishes the ability of these cancer cells to form colonies in a dose-dependent fashion. It acts as a powerful suppressor of lipogenic gene activity, uniquely eliminating cancer cells by depleting their lipid content. The presence of oleate, stearate, and palmitate together in the culture medium fully restores the viability of these cancer cells. Additionally, supplementing with fatty acids revives SW620 cells' viability, particularly where glycolysis is greatly impaired^[1].