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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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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.
| Targets |
Liver-X-receptor (LXR)
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| 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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| Enzyme Assay |
Biochemical NR-Cofactor Peptide Interaction (TR-FRET) Assay: Assay was carried out as previously described(Griffett et al., 2013). Sequences used for this assay are as follows. NCoR ID1 Sequence: Fluorescein-LITLADHICQIITQ, NCoR ID2 Sequence: Fluorescein-NLGLEDIIRKALMG, SMRT ID2 Fluorescein-HASTNMGLEAIIRKALMGKYDQW, and TRAP220/DRIP-2 Sequence: Fluorescein-NTKNHPMLMNLLKDNPAQD[1].
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| Cell Assay |
Colony Formation Assay: Cancer cells were plated at low-density (5×103) cells per well. Cells were then treated with either DMSO vehicle control, SR9243 (100nM) or SR9243 (10μM) and allowed to grow for 4 days. Colonies were then fixed with Formaldehyde (1%) and stained with Crystal violet solution (0.05% w/v)[1].
Cell Viability/Apoptosis Microscopy Assay: Cells were grown on glass chamber slides (BD Falcon) until 80% confluent. On the day of staining, media was removed and replaced with 1X Nuclear-ID Blue/Green staining reagent in PBS and incubated at 37oC for 30 minutes. Staining reagent was removed and several drops of 1X PBS were added to the cells. The cells were coverslipped and observed under a fluorescence microscope with filters for DAPI and FITC[1]. In vitro Apoptosis Assay: Cancer cells were treated with 100 nM SR9243 for 24 hr in low serum media. Cells were harvested using trypsin as described earlier and stained using Annexin V FITC and Propidium Iodide apoptosis detection kit according to the manufacturer’s instructions then subjected to FACs analysis. |
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| Animal Protocol |
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| References | |||
| Additional Infomation |
SR9243 is a sulfonamide resulting from the formal condensation of the sulfonic acid group of mesitylene-2-sulphonic acid with the amino group of 2-(m-bromophenyl)ethylamine in which the nitrogen is substituted by a 4-[m-(methylsulfonyl)phenyl]benzyl group. It has a role as an antineoplastic agent, an apoptosis inducer and a liver X receptor inverse agonist. It is a sulfonamide, a sulfone and a member of bromobenzenes.
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| Molecular Formula |
C31H32BRNO4S2
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| Molecular Weight |
626.62
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| Exact Mass |
625.095
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| Elemental Analysis |
C, 59.42; H, 5.15; Br, 12.75; N, 2.24; O, 10.21; S, 10.23
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| CAS # |
1613028-81-1
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| Related CAS # |
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| PubChem CID |
76073169
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| Appearance |
Typically exists as white to off-white solids at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
786.3±70.0 °C at 760 mmHg
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| Flash Point |
429.3±35.7 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.616
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| LogP |
7.72
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
39
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| Complexity |
971
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| Defined Atom Stereocenter Count |
0
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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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| HS Tariff Code |
2934.99.9001
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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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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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