SR9243 is a potent and selective LXR inverse agonist. 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. In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression. SR9243 induced apoptosis in tumors without inducing weight loss, hepatotoxicity, or inflammation. Malignant cells exhibit aerobic glycolysis (the Warburg effect) and become dependent on de novo lipogenesis, which sustains rapid proliferation and resistance to cellular stress.
CAS Number: 1613028-81-1
Molecular Weight: 626.62
Chemical Name: N-(3-bromophenethyl)-2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)benzenesulfonamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
SR9243 was used at 1-10 µM final concentration in vitro and in cellular assays.
SR9243 was dosed to mice bearing SW620, DU-145 and LLC cells subcutaneous xenografts at 60 mg/kg once per day.
- Flaveny CA, et al. Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. (2015) Cancer Cell. 28(1):42-56.
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