MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

iNOS:158 nM

MSU-42011 (300 nM; 8 h) showed a low induction effect on SREBP in HepG2 cells.[1]
MSU-42011 (0-5000 nM; 24 h) can activate RXR in HepG2 cells.[1]

MSU-42011 (25 mg/kg; oral; for 12 weeks) significantly reduced the number, size, and overall tumor burden of tumors in the A/J mouse lung cancer model. Compared with the control group, there were fewer cells with active proliferation and showed a significant decrease in p-ERK [1].
MSU-42011 (25 mg/kg; oral; single dose) is most effective in reducing the number, size, and overall tumor burden of the A/J mouse lung cancer model in combination with C/P. Reduced macrophages in the lungs and increased activation markers of CD8+T cells [1].
MSU42011 (100 mg/kg; PO; single dose) reduces tumor burden in a mouse lung tumor model [2].