LG100268

LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC₅₀ values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively^[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the K_i values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively^[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy^[3]. In Vitro: LG100268 (100 nM-1 μM; 24 hours) shows a downregulation of CSF3 and a 2.5-fold decrease of CXCL2 and IL-1β mRNA expression in RAW264.7 cells^[3].
In Vivo: LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) combines with C/P presents a more markedly reduced average tumor burden than LG268 or C/P alone. The combination establish a reduced lung tumors, which represents a reduction of 82% (vs. 59%-67% with the single drugs) in comparison with the controls^[3].