| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
PPARγ
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|---|---|
| ln Vivo |
In a UMUC9 UC xenograft mouse model, FX-909 (0.03-1 mg/kg; BID for 21 days) has anti-cancer properties [1].
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| References | |
| Additional Infomation |
PPAR Gamma Inhibitor FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator-activated receptor gamma (PPAR gamma; PPARG), with potential antineoplastic activity. Upon oral administration, PPARG inhibitor FX-909 selectively targets and covalently binds to a region of PPARG that is sequestered from the mutation site. The binding promotes a repressive conformation of PPARG and inhibits the activity of PPARG. This inhibits both basal- and ligand-activated transcription by PPARG and prevents PPARG-mediated transcription of target genes, such as FABP4/Fabp4, AGT/Agt, IVT/Ivd and ARG1/Arg1. This may inhibit proliferation in PPARG-overactivated tumor cells. PPARG, a nuclear receptor, is genetically altered, including amplification, missense mutations, and fusions, in certain tumor cells commonly associated with the luminal lineage subtype.
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| Molecular Formula |
C17H10F2N2O3S
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|---|---|
| Molecular Weight |
360.334709644318
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| Exact Mass |
360.038
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| CAS # |
2924573-90-8
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| PubChem CID |
167993670
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
737
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(F)C=C2C(=C(F)C=1)C(=O)C=C(C1=C(C=CC(C#N)=C1)S(=O)(=O)C)N2
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| InChi Key |
RBUBBZVQPHSZEZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H10F2N2O3S/c1-25(23,24)16-3-2-9(8-20)4-11(16)13-7-15(22)17-12(19)5-10(18)6-14(17)21-13/h2-7H,1H3,(H,21,22)
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| Chemical Name |
3-(5,7-difluoro-4-oxo-1H-quinolin-2-yl)-4-methylsulfonylbenzonitrile
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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 |
| 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) |
DMSO: 100 mg/mL (277.52 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7752 mL | 13.8762 mL | 27.7523 mL | |
| 5 mM | 0.5550 mL | 2.7752 mL | 5.5505 mL | |
| 10 mM | 0.2775 mL | 1.3876 mL | 2.7752 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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