| Bioactivity | 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 Ki 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]. | ||||||||||||
| Invitro | 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]. Cell Viability Assay[3] Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | LG100268 | ||||||||||||
| CAS | 153559-76-3 | ||||||||||||
| Formula | C24H29NO2 | ||||||||||||
| Molar Mass | 363.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. M F Boehm, et al. Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. J Med Chem [2]. D S Lala, et al. Activation of Specific RXR Heterodimers by an Antagonist of RXR Homodimers.Nature. 1996 Oct 3;383(6599):450-3. [3]. Martine Cao,et al.The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice. Cancer Prev Res (Phila). 2016 Jan;9(1):105-14. |