product name SR9243
Description: SR9243 is a potent and selective inverse agonist of LXR. It potently reduces cancer cell viability (IC50=15–104 nM) in MTT reduction assays in prostate (PC3 and DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. SR9243 kills cancer cells by inhibiting lipid production and the Warburg effect. SR9243 induces cell death in multiple types of cancer and does not cause the side effects that have derailed previous attempts to target these processes.
References: Cancer Cell. 2015 Jul 13;28(1):42-56.
626.62
Formula
C31H32BrNO4S2
CAS No.
1613028-81-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In HEK293 cells expressing LXRs, SR9243 inhibits LXR activation by enhancing LXR-corepressor recruitment. In a variety of cancer cell types, SR9243 reduces cancer cell viability, induces apoptotic cell death, and sensitizes cancer cells to chemotherapeutic treatments. Kinase Assay: Cell Assay: Cells are cultured in 96 well plates and treated with designated amounts of SR9243 for 96 hr in media containing 1% FBS and antibiotics. Cell-viability is assessed using the Cell-titre 96 kit according to the manufacturer’s guidelines. Cell culture media is supplemented with oleate, stearate and palmitate dissolved in methanol to a concentration of 25 mM. 25 mM stocks are then diluted 10 fold in PBS containing 0.9% BSA. Lipid stocks (100X) are stored at −20° until needed. |
|---|---|
| In Vivo | In Ob/Ob mice fed a high-fat diet, SR9243 (60 mg/kg, i.p.) inhibits LXR-dependent lipogenic enzyme gene expression and tumor growth. |
| Animal model | Mice bearing SW620, DU-145, or LLC tumors |
| Formulation & Dosage | Formulated in 10% DMSO, 10% Tween-80; 30, 60 mg/kg, once daily; i.p. injection |
| References | Cancer Cell. 2015 Jul 13;28(1):42-56. |
