MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist.MSU-42011 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.MSU-42011 is an effective therapy for the treatment of preclinical krasdriven lung cancer and has immunomodulatory activity.

iNOS:158 nM

MSU-42011（300 nM；8小时）在HepG2细胞中对SREBP的诱导效果较低。[1] MSU-42011（0-5000 nM；24小时）能够在HepG2细胞中激活RXR。[1]

MSU-42011 (25 mg/kg；口服；持续12周) 在A/J小鼠肺癌模型中，显著地减少了肿瘤的数量、大小及总体肿瘤负担。与对照组相比，具有活跃增殖的细胞数量减少，并且在p-ERK[1]上表现出显著下降。MSU-42011（25 mg/kg；口服；单次剂量）与C/P联合使用时，能有效地降低A/J小鼠肺癌模型中的肿瘤数量、大小及总体肿瘤负担，减少肺部巨噬细胞，并增加CD8+T细胞激活标志物的表达[1]。MSU42011（100 mg/kg；PO；单次剂量）能减轻小鼠肺肿瘤模型中的肿瘤负担[2]。