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Purity: ≥98%
SR9243 (SR-9243) 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.
| ln Vitro |
Targeting LXR specifically, SR9243 downregulates LXR-mediated gene expression, efficiently suppresses LXR-driven luciferase activity in grown cancer cells, and in a dose-dependent manner at nanomolar concentrations, inhibits LXRα and LXRβ-dependent transcription. In cancer cell lines from the prostate (PC3, DU-145), colon (SW620 and HT29), lung (HOP-62 and NCI-H23), and other organs, SR9243 suppresses cell viability. Additionally, SR9243 dramatically and dose-dependently decreased the capacity of cancer cells to form colonies. By reducing intracellular lipid levels, SR9243, a strong inhibitor of adipogenesis gene expression, specifically kills cancer cells. Oleate, stearate, and palmitate combined with cancer cell growth media totally restored the vitality of cancer cells. Fatty acid supplementation can help restore the viability of SW620 cells when glycolysis is severely impaired [1].
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| ln Vivo |
In vivo, SR9243 causes apoptotic cancer cell death, dramatically reduces tumor glycolysis and lipogenesis, and does not increase weight loss. Without causing hepatotoxicity or inflammation, SR9243 suppresses tumor development and lipogenesis in vivo by negating the expression of glycolytic genes to a large extent [1].
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| Animal Protocol |
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| References |
[1]. Flaveny CA, et al. Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer Cell. 2015 Jun 24. pii: S1535-6108(15)00183-X
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| Molecular Formula |
C31H32BRNO4S2
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| Molecular Weight |
626.62
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| CAS # |
1613028-81-1
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| Related CAS # |
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| SMILES |
BrC1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])C([H])([H])N(C([H])([H])C1C([H])=C([H])C(C2C([H])=C([H])C([H])=C(C=2[H])S(C([H])([H])[H])(=O)=O)=C([H])C=1[H])S(C1C(C([H])([H])[H])=C([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])[H])(=O)=O
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| InChi Key |
InChI=1S/C31H32BrNO4S2/c1-22-17-23(2)31(24(3)18-22)39(36,37)33(16-15-25-7-5-9-29(32)19-25)21-26-11-13-27(14-12-26)28-8-6-10-30(20-28)38(4,34)35/h5-14,17-20H,15-16,21H2,1-4H3
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| InChi Code |
FYQFEJFTCLKXTQ-UHFFFAOYSA-N
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| Chemical Name |
N-(3-bromophenethyl)-2,4,6-trimethyl-N-((3-(methylsulfonyl)-[1,1-biphenyl]-4-yl)methyl)benzenesulfonamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5959 mL | 7.9793 mL | 15.9586 mL | |
| 5 mM | 0.3192 mL | 1.5959 mL | 3.1917 mL | |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5959 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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